200,000+ products from a single source!

sales@angenechem.com

Home > Other Building Blocks > 186692-46-6

186692-46-6

186692-46-6 | Roscovitine

CAS No: 186692-46-6 Catalog No: AG003U50 MDL No:MFCD02266401

Product Description

Catalog Number:
AG003U50
Chemical Name:
Roscovitine
CAS Number:
186692-46-6
Molecular Formula:
C19H26N6O
Molecular Weight:
354.4493
MDL Number:
MFCD02266401
IUPAC Name:
(2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol
InChI:
InChI=1S/C19H26N6O/c1-4-15(11-26)22-19-23-17(20-10-14-8-6-5-7-9-14)16-18(24-19)25(12-21-16)13(2)3/h5-9,12-13,15,26H,4,10-11H2,1-3H3,(H2,20,22,23,24)/t15-/m1/s1
InChI Key:
BTIHMVBBUGXLCJ-OAHLLOKOSA-N
SMILES:
CC[C@@H](Nc1nc(NCc2ccccc2)c2c(n1)n(cn2)C(C)C)CO
UNII:
0ES1C2KQ94
NSC Number:
701554

Properties

Complexity:
417  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Defined Bond Stereocenter Count:
0
Exact Mass:
354.217g/mol
Formal Charge:
0
Heavy Atom Count:
26  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0
Molecular Weight:
354.458g/mol
Monoisotopic Mass:
354.217g/mol
Rotatable Bond Count:
8  
Topological Polar Surface Area:
87.9A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
3.2  

Literature

Title Journal
Neurotrophins and cholinergic enzyme regulated by calpain-2: New insights into neuronal apoptosis induced by polybrominated diphenyl ether-153. Toxicology letters 20180701
Calpain-2/p35-p25/Cdk5 pathway is involved in the neuronal apoptosis induced by polybrominated diphenyl ether-153. Toxicology letters 20170805
Aryl hydrocarbon receptor-dependent up-regulation of the heterodimeric amino acid transporter LAT1 (SLC7A5)/CD98hc (SLC3A2) by diesel exhaust particle extract in human bronchial epithelial cells. Toxicology and applied pharmacology 20160101
Synergism of cyclin-dependent kinase inhibitors with camptothecin derivatives in small cell lung cancer cell lines. Molecules (Basel, Switzerland) 20140217
Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorganic & medicinal chemistry letters 20130801
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. The Biochemical journal 20130415
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. Journal of medicinal chemistry 20130214
Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia cells. BMC pharmacology & toxicology 20130101
Reversal of BoNT/A-mediated inhibition of muscle paralysis by 3,4-diaminopyridine and roscovitine in mouse phrenic nerve-hemidiaphragm preparations. Neurochemistry international 20121101
Roscovitine is a novel agent that can be used for the activation of porcine oocytes reconstructed with adult cutaneous or fetal fibroblast cell nuclei. Theriogenology 20121101
Use of ATP analogs to inhibit HIV-1 transcription. Virology 20121010
Regulation of pregnane X receptor (PXR) function and UGT1A1 gene expression by posttranslational modification of PXR protein. Drug metabolism and disposition: the biological fate of chemicals 20121001
In vivo vs. in vitro models for studying the effects of elevated temperature on the GV-stage oocyte, subsequent developmental competence and gene expression. Animal reproduction science 20121001
Can ex vivo evaluation (testing) predict the sensitivity of CLL cells to therapy with purine analogs in conjunction with an alkylating agent? A comparison of in vivo and ex vivo responses to treatment. Medical oncology (Northwood, London, England) 20120901
Dephosphorylation of threonine-821 of the retinoblastoma tumor suppressor protein (Rb) is required for apoptosis induced by UV and Cdk inhibition. Cell cycle (Georgetown, Tex.) 20120901
Ryanodine receptor blockade reduces amyloid-β load and memory impairments in Tg2576 mouse model of Alzheimer disease. The Journal of neuroscience : the official journal of the Society for Neuroscience 20120822
Activation of Aurora-A is essential for neuronal migration via modulation of microtubule organization. The Journal of neuroscience : the official journal of the Society for Neuroscience 20120808
[Ca2+]i rise at in vitro maturation in bovine cumulus-oocyte complexes. Molecular reproduction and development 20120601
Inhibition of ornithine decarboxylase alters the roscovitine-induced mitochondrial-mediated apoptosis in MCF-7 breast cancer cells. Molecular medicine reports 20120501
Domain III regulates N-type (CaV2.2) calcium channel closing kinetics. Journal of neurophysiology 20120401
Silencing of the polyamine catabolic key enzyme SSAT prevents CDK inhibitor-induced apoptosis in Caco-2 colon cancer cells. Molecular medicine reports 20120401
Synapsin selectively controls the mobility of resting pool vesicles at hippocampal terminals. The Journal of neuroscience : the official journal of the Society for Neuroscience 20120321
Cdk5 protein inhibition and Aβ42 increase BACE1 protein level in primary neurons by a post-transcriptional mechanism: implications of CDK5 as a therapeutic target for Alzheimer disease. The Journal of biological chemistry 20120302
Small molecule screening identifies targetable zebrafish pigmentation pathways. Pigment cell & melanoma research 20120301
LMW-E/CDK2 deregulates acinar morphogenesis, induces tumorigenesis, and associates with the activated b-Raf-ERK1/2-mTOR pathway in breast cancer patients. PLoS genetics 20120301
γ-Aminobutyric acid type A (GABAA) receptor activation modulates tau phosphorylation. The Journal of biological chemistry 20120224
Cdk5 mediates vimentin Ser56 phosphorylation during GTP-induced secretion by neutrophils. Journal of cellular physiology 20120201
Polyamine depletion enhances the roscovitine-induced apoptosis through the activation of mitochondria in HCT116 colon carcinoma cells. Amino acids 20120201
Roscovitine inhibits CaV3.1 (T-type) channels by preferentially affecting closed-state inactivation. The Journal of pharmacology and experimental therapeutics 20120201
Heterogeneous reallocation of presynaptic efficacy in recurrent excitatory circuits adapting to inactivity. Nature neuroscience 20120201
The cyclin-dependent kinase inhibitor p57(Kip2) is epigenetically regulated in carboplatin resistance and results in collateral sensitivity to the CDK inhibitor seliciclib in ovarian cancer. British journal of cancer 20120131
GSK3β inhibition is involved in the neuroprotective effects of cyclin-dependent kinase inhibitors in neurons. Pharmacological research 20120101
Mechanism-based therapeutics for autosomal dominant polycystic kidney disease: recent progress and future prospects. Nephron. Clinical practice 20120101
Cyclin-dependent kinase 9 activity regulates neutrophil spontaneous apoptosis. PloS one 20120101
Polo Like Kinase 2 Tumour Suppressor and cancer biomarker: new perspectives on drug sensitivity/resistance in ovarian cancer. Oncotarget 20120101
Ser-634 and Ser-636 of Kaposi's Sarcoma-Associated Herpesvirus RTA are Involved in Transactivation and are Potential Cdk9 Phosphorylation Sites. Frontiers in microbiology 20120101
Pharmacodynamic modelling of biomarker data in oncology. ISRN pharmacology 20120101
Characterization of cyclin E expression in multiple myeloma and its functional role in seliciclib-induced apoptotic cell death. PloS one 20120101
R-roscovitine reduces lung inflammation induced by lipoteichoic acid and Streptococcus pneumoniae. Molecular medicine (Cambridge, Mass.) 20120101
Enhancement of carboplatin- and quercetin-induced cell death by roscovitine is Akt dependent and p53 independent in hepatoma cells. Integrative cancer therapies 20111201
Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors. European journal of medicinal chemistry 20111201
Using iPSC-derived neurons to uncover cellular phenotypes associated with Timothy syndrome. Nature medicine 20111201
Cyclic AMP induces IPC leukemia cell apoptosis via CRE-and CDK-dependent Bim transcription. Cell death & disease 20111201
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. Bioorganic & medicinal chemistry 20111115
Synthesis and biological evaluation of new 3-(6-hydroxyindol-2-yl)-5-(Phenyl) pyridine or pyrazine V-Shaped molecules as kinase inhibitors and cytotoxic agents. European journal of medicinal chemistry 20111101
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nature biotechnology 20111101
Small molecule cyclin-dependent kinase inhibitors protect against neuronal cell death in the ischemic-reperfused rat retina. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics 20111001
Anti-angiogenic effects of purine inhibitors of cyclin dependent kinases. Angiogenesis 20110901
Quercetin downregulates Mcl-1 by acting on mRNA stability and protein degradation. British journal of cancer 20110712
Transcriptional modulation of apoptosis regulators by roscovitine and related compounds. Apoptosis : an international journal on programmed cell death 20110701
Apoptosis induced by overall metabolic stress converges on the Bcl-2 family proteins Noxa and Mcl-1. Apoptosis : an international journal on programmed cell death 20110701
Novel purine-based fluoroaryl-1,2,3-triazoles as neuroprotecting agents: synthesis, neuronal cell culture investigations, and CDK5 docking studies. Bioorganic & medicinal chemistry letters 20110701
Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. Journal of medicinal chemistry 20110623
New insights into the control of HIV-1 transcription: when Tat meets the 7SK snRNP and super elongation complex (SEC). Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology 20110601
Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity. European journal of medicinal chemistry 20110601
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. European journal of medicinal chemistry 20110601
Meiotic inhibition of bovine oocytes in medium supplemented with a serum replacer and hormones: effects on meiosis progression and developmental capacity. Zygote (Cambridge, England) 20110501
Activation of AMP-activated protein kinase may not be involved in AICAR- and metformin-mediated meiotic arrest in bovine denuded and cumulus-enclosed oocytes in vitro. Zygote (Cambridge, England) 20110501
Raman micro-spectroscopic analysis of cultured HCT116 colon cancer cells in the presence of roscovitine. Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy 20110501
Antiapoptotic effects of roscovitine on camptothecin-induced DNA damage in neuroblastoma cells. Apoptosis : an international journal on programmed cell death 20110501
Treatment with a cyclin-dependent kinase inhibitor, seliciclib, is effective in reducing glomerular macrophage numbers and the severity of established experimental glomerulonephritis. Nephrology (Carlton, Vic.) 20110501
A bioinformatical and functional approach to identify novel strategies for chemoprevention of colorectal cancer. Oncogene 20110428
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity. Journal of medicinal chemistry 20110428
Alterations of cyclin dependent kinase 5 expression and phosphorylation in amyloid precursor protein (APP)-transfected PC12 cells. FEBS letters 20110420
Fluorescent cyclin-dependent kinase inhibitors block the proliferation of human breast cancer cells. Bioorganic & medicinal chemistry 20110415
Androgen stimulates endothelial cell proliferation via an androgen receptor/VEGF/cyclin A-mediated mechanism. American journal of physiology. Heart and circulatory physiology 20110401
Interference with ER-α enhances the therapeutic efficacy of the selective CDK inhibitor roscovitine towards ER-positive breast cancer cells. Journal of cellular biochemistry 20110401
Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors. Bioorganic & medicinal chemistry letters 20110401
High throughput screens yield small molecule inhibitors of Leishmania CRK3:CYC6 cyclin-dependent kinase. PLoS neglected tropical diseases 20110401
Immunodetection of retinoblastoma-related protein and its phosphorylated form in interphase and mitotic alfalfa cells. Journal of experimental botany 20110301
Roscovitine, a selective CDK inhibitor, reduces the basal and estrogen-induced phosphorylation of ER-α in human ER-positive breast cancer cells. Journal of cellular biochemistry 20110301
p38 phosphorylates Rb on Ser567 by a novel, cell cycle-independent mechanism that triggers Rb-Hdm2 interaction and apoptosis. Oncogene 20110203
6-Hydroxydopamine-induced PC12 cell death is mediated by MEF2D down-regulation. Neurochemical research 20110201
Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25. Bioorganic & medicinal chemistry 20110101
Liposarcoma: molecular genetics and therapeutics. Sarcoma 20110101
Effect of anti-estrogen combined with roscovitine, a selective CDK inhibitor, on human breast cancer cells differing in expression of ER. Journal of experimental therapeutics & oncology 20110101
Tamoxifen enhances the anti-proliferative effect of roscovitine, a selective cyclin-dependent kinase inhibitor, on human ER-positive human breast cancer cells. Journal of experimental therapeutics & oncology 20110101
WEE1 inhibition sensitizes osteosarcoma to radiotherapy. BMC cancer 20110101
Limited redundancy in genes regulated by Cyclin T2 and Cyclin T1. BMC research notes 20110101
Differential inhibitor sensitivity between human kinases VRK1 and VRK2. PloS one 20110101
Roscovitine confers tumor suppressive effect on therapy-resistant breast tumor cells. Breast cancer research : BCR 20110101
Quercetin suppresses cyclooxygenase-2 expression and angiogenesis through inactivation of P300 signaling. PloS one 20110101
Antitumor activity of a novel oncrasin analogue is mediated by JNK activation and STAT3 inhibition. PloS one 20110101
The Role of RNA Polymerase II Elongation Control in HIV-1 Gene Expression, Replication, and Latency. Genetics research international 20110101
Targeting apoptosis signaling pathways for anticancer therapy. Frontiers in oncology 20110101
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. Journal of medicinal chemistry 20101223
Time course of in vitro maturation of compact cumulus horse oocytes after roscovitine-induced meiotic inhibition: effects on the coordination between nuclear and cytoplasmic maturation. Reproduction in domestic animals = Zuchthygiene 20101201
Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies. European journal of cancer (Oxford, England : 1990) 20101201
Cyclin-dependent kinase 5 regulates endothelial cell migration and angiogenesis. The Journal of biological chemistry 20101112
Regulation of C/EBPbeta1 by Ras in mammary epithelial cells and the role of C/EBPbeta1 in oncogene-induced senescence. Oncogene 20101111
ATP-binding cassette B1 transports seliciclib (R-roscovitine), a cyclin-dependent kinase inhibitor. Drug metabolism and disposition: the biological fate of chemicals 20101101
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. Bioorganic & medicinal chemistry letters 20101101
Inhibition of MCL-1 in breast cancer cells promotes cell death in vitro and in vivo. Cancer biology & therapy 20101101
Combination of sapacitabine and HDAC inhibitors stimulates cell death in AML and other tumour types. British journal of cancer 20101026
Roscovitine-based CDK inhibitors acting as N-donor ligands in the platinum(II) oxalato complexes: preparation, characterization and in vitro cytotoxicity. European journal of medicinal chemistry 20101001
Chemotherapy-induced genotoxic stress promotes sensitivity to natural killer cell cytotoxicity by enabling missing-self recognition. Cancer research 20100915
CDK5 serves as a major control point in neurotransmitter release. Neuron 20100909
Role of NOXA and its ubiquitination in proteasome inhibitor-induced apoptosis in chronic lymphocytic leukemia cells. Haematologica 20100901
Parthenogenetic development of domestic cat oocytes treated with ionomycin, cycloheximide, roscovitine and strontium. Theriogenology 20100901
Cyclin-dependent kinase activity controls the onset of the HCMV lytic cycle. PLoS pathogens 20100901
Use of a Piezo drill for intracytoplasmic sperm injection into cattle oocytes activated with ionomycin associated with roscovitine. Reproduction in domestic animals = Zuchthygiene 20100801
Regulation of GSK-3beta by calpain in the 3-nitropropionic acid model. Hippocampus 20100801
Probing the probes: fitness factors for small molecule tools. Chemistry & biology 20100625
Strong inhibition of replicative DNA synthesis in the developing rat cerebral cortex and glioma cells by roscovitine. Investigational new drugs 20100601
Microtubule distribution in somatic cell nuclear transfer bovine embryos following control of nuclear remodeling type. Journal of veterinary science 20100601
Effect of cdk5 antagonist on L-dopa-induced dyskinesias in a rat model of Parkinson's disease. The International journal of neuroscience 20100601
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. Journal of medicinal chemistry 20100513
Proliferative suppression by CDK4/6 inhibition: complex function of the retinoblastoma pathway in liver tissue and hepatoma cells. Gastroenterology 20100501
Cyclin-dependent kinase 5 modulates the transcriptional activity of the mineralocorticoid receptor and regulates expression of brain-derived neurotrophic factor. Molecular endocrinology (Baltimore, Md.) 20100501
Graphic rule for drug metabolism systems. Current drug metabolism 20100501
Targeting the cell cycle and the PI3K pathway: a possible universal strategy to reactivate innate tumor suppressor programmes in cancer cells. International journal of oncology 20100401
Dissecting the factors involved in the locomotion mode of neuronal migration in the developing cerebral cortex. The Journal of biological chemistry 20100219
Low-molecular-weight cyclin E can bypass letrozole-induced G1 arrest in human breast cancer cells and tumors. Clinical cancer research : an official journal of the American Association for Cancer Research 20100215
Pivotal Advance: Pharmacological manipulation of inflammation resolution during spontaneously resolving tissue neutrophilia in the zebrafish. Journal of leukocyte biology 20100201
A novel roscovitine derivative potently induces G1-phase arrest in platelet-derived growth factor-BB-activated vascular smooth muscle cells. Molecular pharmacology 20100201
Cyclin-dependent kinase 5 phosphorylates endothelial nitric oxide synthase at serine 116. Hypertension (Dallas, Tex. : 1979) 20100201
Editorial: Maintaining the balance--fishing for drugs to treat persistent neutrophilic inflammation. Journal of leukocyte biology 20100201
C-fin: a cultured frog tadpole tail fin biopsy approach for detection of thyroid hormone-disrupting chemicals. Environmental toxicology and chemistry 20100201
Roscovitine increases intracellular calcium release and capacitative calcium entry in PC12 cells. Neuroscience letters 20100118
Induction of UGT1A1 and CYP2B6 by an antimitogenic factor in HepG2 cells is mediated through suppression of cyclin-dependent kinase 2 activity: cell cycle-dependent expression. Drug metabolism and disposition: the biological fate of chemicals 20100101
Roscovitine binds to novel L-channel (CaV1.2) sites that separately affect activation and inactivation. The Journal of biological chemistry 20100101
RNA polymerase II C-terminal heptarepeat domain Ser-7 phosphorylation is established in a mediator-dependent fashion. The Journal of biological chemistry 20100101
R-roscovitine (Seliciclib) affects CLL cells more strongly than combinations of fludarabine or cladribine with cyclophosphamide: Inhibition of CDK7 sensitizes leukemic cells to caspase-dependent apoptosis. Journal of cellular biochemistry 20100101
Healthy clocks, healthy body, healthy mind. Trends in cell biology 20100101
Targeting the cyclin E-Cdk-2 complex represses lung cancer growth by triggering anaphase catastrophe. Clinical cancer research : an official journal of the American Association for Cancer Research 20100101
The radiosensitising effect of olomoucine derived synthetic cyclin-dependent kinase inhibitors. Neoplasma 20100101
Protection of p53 wild type cells from taxol by nutlin-3 in the combined lung cancer treatment. BMC cancer 20100101
Role of senescence and mitotic catastrophe in cancer therapy. Cell division 20100101
Inhibition of human immunodeficiency virus type-1 by cdk inhibitors. AIDS research and therapy 20100101
In cystic fibrosis homozygotes and heterozygotes, neutrophil apoptosis is delayed and modulated by diamide or roscovitine: evidence for an innate neutrophil disturbance. Journal of innate immunity 20100101
Caffeine prevents transcription inhibition and P-TEFb/7SK dissociation following UV-induced DNA damage. PloS one 20100101
R-Roscovitine (Seliciclib) prevents DNA damage-induced cyclin A1 upregulation and hinders non-homologous end-joining (NHEJ) DNA repair. Molecular cancer 20100101
Delayed treatment with systemic (S)-roscovitine provides neuroprotection and inhibits in vivo CDK5 activity increase in animal stroke models. PloS one 20100101
Application of new drugs in chronic lymphocytic leukemia. Mediterranean journal of hematology and infectious diseases 20100101
Wortmannin potentiates roscovitine-induced growth inhibition in human solid tumor cells by repressing PI3K/Akt pathway. Cancer letters 20091228
Regulation of serotonin 1B receptor by glycogen synthase kinase-3. Molecular pharmacology 20091201
Seliciclib in malignancies. Expert opinion on investigational drugs 20091201
Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology 20091101
Increased expression of androgen receptor sensitizes prostate cancer cells to low levels of androgens. Cancer research 20091015
Cyclin-dependent kinase 5 inhibitors: inhibition of dopamine transporter activity. Molecular pharmacology 20091001
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Nature chemical biology 20091001
Inhibition of CDKS by roscovitine suppressed LPS-induced *NO production through inhibiting NFkappaB activation and BH4 biosynthesis in macrophages. American journal of physiology. Cell physiology 20090901
Cdk2 plays a critical role in hepatocyte cell cycle progression and survival in the setting of cyclin D1 expression in vivo. Cell cycle (Georgetown, Tex.) 20090901
Roscovitine triggers apoptosis in B-cell chronic lymphocytic leukemia cells with similar efficiency as combinations of conventional purine analogs with cyclophosphamide. Annals of the New York Academy of Sciences 20090801
Selective cyclin-dependent kinase inhibitors discriminating between cell cycle and transcriptional kinases: future reality or utopia? Annals of the New York Academy of Sciences 20090801
Roscovitine differentially affects asynchronously growing and synchronized human MCF-7 breast cancer cells. Annals of the New York Academy of Sciences 20090801
Monitoring of long-term effects of resveratrol on cell cycle progression of human HeLa cells after administration of a single dose. Annals of the New York Academy of Sciences 20090801
Liver circadian clock, a pharmacologic target of cyclin-dependent kinase inhibitor seliciclib. Chronobiology international 20090801
The Cdk5 inhibitor roscovitine strongly inhibits glucose uptake in 3T3-L1 adipocytes without altering GLUT4 translocation from internal pools to the cell surface. Journal of cellular physiology 20090701
Cell cycle inhibition attenuates microglial proliferation and production of IL-1beta, MIP-1alpha, and NO after focal cerebral ischemia in the rat. Glia 20090601
Functional p53 in cells contributes to the anticancer effect of the cyclin-dependent kinase inhibitor roscovitine. Journal of cellular biochemistry 20090601
Therapeutic efficacy of seliciclib in combination with ionizing radiation for human nasopharyngeal carcinoma. Clinical cancer research : an official journal of the American Association for Cancer Research 20090601
Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood 20090507
Off-target decoding of a multitarget kinase inhibitor by chemical proteomics. Chembiochem : a European journal of chemical biology 20090504
The cyclin-dependent kinase inhibitor roscovitine and the nucleoside analog sangivamycin induce apoptosis in caspase-3 deficient breast cancer cells independent of caspase mediated P-glycoprotein cleavage: implications for therapy of drug resistant breast cancers. Cell cycle (Georgetown, Tex.) 20090501
Talin phosphorylation by Cdk5 regulates Smurf1-mediated talin head ubiquitylation and cell migration. Nature cell biology 20090501
PP1-mediated dephosphorylation of phosphoproteins at mitotic exit is controlled by inhibitor-1 and PP1 phosphorylation. Nature cell biology 20090501
QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors. Bioorganic & medicinal chemistry letters 20090415
Reduced amyloidogenic processing of the amyloid beta-protein precursor by the small-molecule Differentiation Inducing Factor-1. Cellular signalling 20090401
Outcome of treatment of human HeLa cervical cancer cells with roscovitine strongly depends on the dosage and cell cycle status prior to the treatment. Journal of cellular biochemistry 20090401
Inhibition of cyclin-dependent kinases by olomoucine and roscovitine reduces lipopolysaccharide-induced inflammatory responses via down-regulation of nuclear factor kappaB. Cell proliferation 20090401
Regulation of Cdh1-APC function in axon growth by Cdh1 phosphorylation. The Journal of neuroscience : the official journal of the Society for Neuroscience 20090401
Apoptosis of metastatic prostate cancer cells by a combination of cyclin-dependent kinase and AKT inhibitors. The international journal of biochemistry & cell biology 20090301
Colon mustard oil instillation induced cross-organ reflex sensitization on the pelvic-urethra reflex activity in rats. Pain 20090301
Role of the HIV-1 positive elongation factor P-TEFb and inhibitors thereof. Mini reviews in medicinal chemistry 20090301
Development of cell-cycle inhibitors for cancer therapy. Current oncology (Toronto, Ont.) 20090301
Advances in the pathogenesis and treatment of polycystic kidney disease. Current opinion in nephrology and hypertension 20090301
The role of Cdk5 in retinoic acid-induced apoptosis of cervical cancer cell line. The Chinese journal of physiology 20090227
Pharmacodynamic effects of seliciclib, an orally administered cell cycle modulator, in undifferentiated nasopharyngeal cancer. Clinical cancer research : an official journal of the American Association for Cancer Research 20090215
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue. Journal of medicinal chemistry 20090212
Inhibition of glycogen synthase kinase-3beta downregulates total tau proteins in cultured neurons and its reversal by the blockade of protein phosphatase-2A. Brain research 20090203
Cellular phototoxicity evoked through the inhibition of human ABC transporter ABCG2 by cyclin-dependent kinase inhibitors in vitro. Pharmaceutical research 20090201
Cell cycle synchronization of canine ear fibroblasts for somatic cell nuclear transfer. Zygote (Cambridge, England) 20090201
The Timothy syndrome mutation of cardiac CaV1.2 (L-type) channels: multiple altered gating mechanisms and pharmacological restoration of inactivation. The Journal of physiology 20090201
Seliciclib (CYC202, R-roscovitine) enhances the antitumor effect of doxorubicin in vivo in a breast cancer xenograft model. International journal of cancer 20090115
Molecular therapies for systemic lupus erythematosus: clinical trials and future prospects. Arthritis research & therapy 20090101
The cyclin-dependent kinase inhibitor 5, 6-dichloro-1-beta-D-ribofuranosylbenzimidazole induces nongenotoxic, DNA replication-independent apoptosis of normal and leukemic cells, regardless of their p53 status. BMC cancer 20090101
Regulation of HIV-1 transcription in cells of the monocyte-macrophage lineage. Retrovirology 20090101
You never know: Cdk inhibitors as anti-cancer drugs. Cell cycle (Georgetown, Tex.) 20081215
Isothiocyanate NB7M causes selective cytotoxicity, pro-apoptotic signalling and cell-cycle regression in ovarian cancer cells. British journal of cancer 20081202
Action of resveratrol alone or in combination with roscovitine, a CDK inhibitor, on cell cycle progression in human HL-60 leukemia cells. Biochemical pharmacology 20081201
Pleiotropic effects of selective CDK inhibitors on human normal and cancer cells. Biochemical pharmacology 20081201
Small-molecule Bcl-2 antagonists as targeted therapy in oncology. Current oncology (Toronto, Ont.) 20081201
Human cytomegalovirus IE1 protein enhances herpes simplex virus type 1-induced syncytial formation in U373MG cells. Journal of Korean medical science 20081201
Synthesis and biological evaluation of diversely substituted indolin-2-ones. European journal of medicinal chemistry 20081101
Restoration of renal function in zebrafish models of ciliopathies. Pediatric nephrology (Berlin, Germany) 20081101
Role of caspases, calpain and cdk5 in ammonia-induced cell death in developing brain cells. Neurobiology of disease 20081101
The histone-deacetylase inhibitor MS-275 and the CDK-inhibitor CYC-202 promote anti-tumor effects in hepatoma cell lines. Oncology reports 20081101
CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene 20081002
(R)-roscovitine, a cyclin-dependent kinase inhibitor, enhances tonic GABA inhibition in rat hippocampus. Neuroscience 20081002
Autophagy: a novel mechanism of synergistic cytotoxicity between doxorubicin and roscovitine in a sarcoma model. Cancer research 20081001
Activation of Cdk2 stimulates proteasome-dependent truncation of tyrosine phosphatase SHP-1 in human proliferating intestinal epithelial cells. The Journal of biological chemistry 20080912
Roscovitine synergizes with conventional chemo-therapeutic drugs to induce efficient apoptosis of human colorectal cancer cells. World journal of gastroenterology 20080907
N-&-N, a new class of cell death-inducing kinase inhibitors derived from the purine roscovitine. Molecular cancer therapeutics 20080901
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design. Journal of medicinal chemistry 20080828
NMR screening for lead compounds using tryptophan-mutated proteins. Journal of medicinal chemistry 20080828
Mitotic arrest-associated apoptosis induced by sodium arsenite in A375 melanoma cells is BUBR1-dependent. Toxicology and applied pharmacology 20080815
The antiproliferative activity of melatonin in B65 rat dopaminergic neuroblastoma cells is related to the downregulation of cell cycle-related genes. Journal of pineal research 20080801
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies. European journal of medicinal chemistry 20080701
Flow cytometric cell cycle analysis of cultured brown bear fibroblast cells. Cell biology international 20080701
Effect of serum starvation and chemical inhibitors on cell cycle synchronization of canine dermal fibroblasts. Theriogenology 20080701
Synergistic inhibition of ErbB signaling by combined treatment with seliciclib and ErbB-targeting agents. Clinical cancer research : an official journal of the American Association for Cancer Research 20080701
Temporal profiling of the chromatin proteome reveals system-wide responses to replication inhibition. Current biology : CB 20080603
Effect of seliciclib (CYC202, R-roscovitine) on lymphocyte alloreactivity and acute kidney allograft rejection in rat. Transplantation 20080527
The separation of antagonist from agonist effects of trisubstituted purines on CaV2.2 (N-type) channels. Journal of neurochemistry 20080501
cdc2-cyclin B regulates eEF2 kinase activity in a cell cycle- and amino acid-dependent manner. The EMBO journal 20080409
Resveratrol modulates roscovitine-mediated cell cycle arrest of human MCF-7 breast cancer cells. Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association 20080401
Butyrolactone I derivatives from Aspergillus terreus carrying an unusual sulfate moiety. Journal of natural products 20080401
Chemical activation of in vitro matured dromedary camel (Camelus dromedarius) oocytes: optimization of protocols. Theriogenology 20080315
Nuclear maturation kinetics and in vitro embryo development of cattle oocytes prematured with butyrolactone I combined or not combined with roscovitine. Animal reproduction science 20080303
Metabolism of the trisubstituted purine cyclin-dependent kinase inhibitor seliciclib (R-roscovitine) in vitro and in vivo. Drug metabolism and disposition: the biological fate of chemicals 20080301
Spatio-temporal expression patterns of aurora kinases a, B, and C and cytoplasmic polyadenylation-element-binding protein in bovine oocytes during meiotic maturation. Biology of reproduction 20080201
Polycystic kidney diseases: from molecular discoveries to targeted therapeutic strategies. Cellular and molecular life sciences : CMLS 20080201
Cyclin-dependent kinase inhibitor roscovitine induces cell cycle arrest and apoptosis in rabbit retinal pigment epithelial cells. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics 20080201
Phosphatidylcholine biosynthesis via CTP:phosphocholine cytidylyltransferase 2 facilitates neurite outgrowth and branching. The Journal of biological chemistry 20080104
A quantitative analysis of kinase inhibitor selectivity. Nature biotechnology 20080101
Better understanding of ADPKD results in potential new treatment options: ready for the cure? Journal of nephrology 20080101
Lysine methylation of HIV-1 Tat regulates transcriptional activity of the viral LTR. Retrovirology 20080101
Synchronisation of canine germinal vesicle stage oocytes prior to in vitro maturation alters the kinetics of nuclear progression during subsequent resumption of meiosis. Reproduction, fertility, and development 20080101
Induction of cytotoxicity, apoptosis and cell cycle arrest by 1-t-butyl carbamoyl, 7-methyl-indole-3-ethyl isothiocyanate (NB7M) in nervous system cancer cells. Drug design, development and therapy 20080101
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proceedings of the National Academy of Sciences of the United States of America 20071218
The selectivity of protein kinase inhibitors: a further update. The Biochemical journal 20071215
A new, unexpected action of olomoucine, a CDK inhibitor, on normal human cells: up-regulation of CLIMP-63, a cytoskeleton-linking membrane protein. Journal of cellular biochemistry 20071215
The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis. Cell cycle (Georgetown, Tex.) 20071215
Shp2E76K mutant confers cytokine-independent survival of TF-1 myeloid cells by up-regulating Bcl-XL. The Journal of biological chemistry 20071214
Effect of the Cdk-inhibitor roscovitine on mouse hematopoietic progenitors in vivo and in vitro. Cancer chemotherapy and pharmacology 20071101
Regulation of membrane association and kinase activity of Cdk5-p35 by phosphorylation of p35. Journal of neuroscience research 20071101
Crosstalk among Bcl-2 family members in B-CLL: seliciclib acts via the Mcl-1/Noxa axis and gradual exhaustion of Bcl-2 protection. Cell death and differentiation 20071101
Inhibition of farnesyl protein transferase sensitizes human MCF-7 breast cancer cells to roscovitine-mediated cell cycle arrest. Journal of cellular biochemistry 20071015
Major Cdk5-dependent phosphorylation sites of amphiphysin 1 are implicated in the regulation of the membrane binding and endocytosis. Journal of neurochemistry 20070901
Roscovitine in B-chronic lymphocytic leukemia cells: high apoptosis-inducing efficacy and synergism with alemtuzumab independent of the patients' pretreatment status. Haematologica 20070901
Antiproliferative effects of sapacitabine (CYC682), a novel 2'-deoxycytidine-derivative, in human cancer cells. British journal of cancer 20070828
Prime time for polycystic kidney disease: does one shot of roscovitine bring the cure? Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20070801
Production of cloned horse foals using roscovitine-treated donor cells and activation with sperm extract and/or ionomycin. Reproduction (Cambridge, England) 20070801
A Cdk5 inhibitor enhances the induction of insulin secretion by exendin-4 both in vitro and in vivo. The journal of physiological sciences : JPS 20070801
Role of cyclin-dependent kinase 5 in capsaicin-induced cough. European journal of pharmacology 20070702
Cyclin-dependent kinase 5 differentially regulates the transcriptional activity of the glucocorticoid receptor through phosphorylation: clinical implications for the nervous system response to glucocorticoids and stress. Molecular endocrinology (Baltimore, Md.) 20070701
'Seed' analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737. Oncogene 20070607
Rosiglitazone sensitizes MDA-MB-231 breast cancer cells to anti-tumour effects of tumour necrosis factor-alpha, CH11 and CYC202. Endocrine-related cancer 20070601
Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology 20070601
Role of roscovitine and IBMX on kinetics of nuclear and cytoplasmic maturation of bovine oocytes in vitro. Animal reproduction science 20070501
The effects of the CDK inhibitor seliciclib alone or in combination with cisplatin in human uterine sarcoma cell lines. Gynecologic oncology 20070501
Anti-proliferative effects of evodiamine on human prostate cancer cell lines DU145 and PC3. Journal of cellular biochemistry 20070501
Cyclin-dependent kinase inhibition limits glomerulonephritis and extends lifespan of mice with systemic lupus. Arthritis and rheumatism 20070501
[Research on cyclin-dependent kinase inhibitors: state of the art and perspective]. Zhonghua zhong liu za zhi [Chinese journal of oncology] 20070501
Mitotic control of RUNX2 phosphorylation by both CDK1/cyclin B kinase and PP1/PP2A phosphatase in osteoblastic cells. Journal of cellular biochemistry 20070415
AKT and CDK5/p35 mediate brain-derived neurotrophic factor induction of DARPP-32 in medium size spiny neurons in vitro. The Journal of biological chemistry 20070309
Studies on cell-cycle synchronization in the asexual erythrocytic stages of Plasmodium falciparum. Parasitology 20070301
Roscovitine-activated HIP2 kinase induces phosphorylation of wt p53 at Ser-46 in human MCF-7 breast cancer cells. Journal of cellular biochemistry 20070301
Paclitaxel induced apoptosis in breast cancer cells requires cell cycle transit but not Cdc2 activity. Cancer chemotherapy and pharmacology 20070201
Roscovitine regulates invasive breast cancer cell (MDA-MB231) proliferation and survival through cell cycle regulatory protein cdk5. Experimental and molecular pathology 20070201
A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days. British journal of cancer 20070115
Mcl-1 down-regulation potentiates ABT-737 lethality by cooperatively inducing Bak activation and Bax translocation. Cancer research 20070115
Study of the inhibition of cyclin-dependent kinases with roscovitine and indirubin-3'-oxime from molecular dynamics simulations. Journal of molecular modeling 20070101
A purine analog kinase inhibitor, calcium/calmodulin-dependent protein kinase II inhibitor 59, reveals a role for calcium/calmodulin-dependent protein kinase II in insulin-stimulated glucose transport. Endocrinology 20070101
Phenol red in the culture medium strongly affects the susceptibility of human MCF-7 cells to roscovitine. Cellular & molecular biology letters 20070101
Cyclin-dependent kinase inhibitor seliciclib shows in vitro activity in diffuse large B-cell lymphomas. Leukemia & lymphoma 20070101
Seliciclib (CYC202; r-roscovitine) in combination with cytotoxic agents in human uterine sarcoma cell lines. Anticancer research 20070101
Effect of distinct anticancer drugs on the phosphorylation of p53 protein at serine 46 in human MCF-7 breast cancer cells. Annals of the New York Academy of Sciences 20070101
Inhibition of HIV-1 replication by P-TEFb inhibitors DRB, seliciclib and flavopiridol correlates with release of free P-TEFb from the large, inactive form of the complex. Retrovirology 20070101
DrugScoreRNA--knowledge-based scoring function to predict RNA-ligand interactions. Journal of chemical information and modeling 20070101
p21 is decreased in polycystic kidney disease and leads to increased epithelial cell cycle progression: roscovitine augments p21 levels. BMC nephrology 20070101
Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology 20070101
Imaging immediate-early and strict-late promoter activity during oncolytic herpes simplex virus type 1 infection and replication in tumors. Gene therapy 20061201
A novel CRM1-dependent nuclear export signal in adenoviral E1A protein regulated by phosphorylation. FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20061201
p21 blocks irradiation-induced apoptosis downstream of mitochondria by inhibition of cyclin-dependent kinase-mediated caspase-9 activation. Cancer research 20061201
Prevention of p53 degradation in human MCF-7 cells by proteasome inhibitors does not mimic the action of roscovitine. Annals of the New York Academy of Sciences 20061201
Improved tumor control through circadian clock induction by Seliciclib, a cyclin-dependent kinase inhibitor. Cancer research 20061115
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. Journal of medicinal chemistry 20061102
Analysis of different factors influencing the intracytoplasmic sperm injection (ICSI) yield in pigs. Theriogenology 20061101
Holding immature equine oocytes in the absence of meiotic inhibitors: effect on germinal vesicle chromatin and blastocyst development after intracytoplasmic sperm injection. Theriogenology 20060901
Enhanced activation of Ca2+/calmodulin-dependent protein kinase II upon downregulation of cyclin-dependent kinase 5-p35. Journal of neuroscience research 20060901
Cyclin-dependent kinase inhibitors enhance the resolution of inflammation by promoting inflammatory cell apoptosis. Nature medicine 20060901
Replication-dependent DNA damage response triggered by roscovitine induces an uncoupling of DNA replication proteins. Cell cycle (Georgetown, Tex.) 20060901
Phenol red reduces ROSC mediated cell cycle arrest and apoptosis in human MCF-7 cells. Journal of cellular biochemistry 20060815
Interplay between the p53 tumor suppressor protein family and Cdk5: novel therapeutic approaches for the treatment of neurodegenerative diseases using selective Cdk inhibitors. Molecular neurobiology 20060801
Cellular stress increases RGS2 mRNA and decreases RGS4 mRNA levels in SH-SY5Y cells. Neuroscience letters 20060724
(R)-roscovitine (CYC202, Seliciclib) sensitizes SH-SY5Y neuroblastoma cells to nutlin-3-induced apoptosis. Experimental cell research 20060715
Cyclin dependent kinase inhibitors prevent apoptosis of postmitotic mouse motoneurons. Life sciences 20060627
The susceptibility of granulosa cells to apoptosis is influenced by oestradiol and the cell cycle. The Journal of endocrinology 20060601
Production of horse foals via direct injection of roscovitine-treated donor cells and activation by injection of sperm extract. Reproduction (Cambridge, England) 20060601
The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction. The European journal of neuroscience 20060601
Interaction energies for the purine inhibitor roscovitine with cyclin-dependent kinase 2: correlated ab initio quantum-chemical, DFT and empirical calculations. Chemistry (Weinheim an der Bergstrasse, Germany) 20060524
In vitro maturation and fertilization of porcine oocytes after a 48 h culture in roscovitine, an inhibitor of p34cdc2/cyclin B kinase. Animal reproduction science 20060501
Developmental competence of bovine oocytes after specific inhibition of MPF kinase activity: effect of estradiol supplementation and follicle size. Animal reproduction science 20060501
Different mechanisms of CDK5 and CDK2 activation as revealed by CDK5/p25 and CDK2/cyclin A dynamics. The Journal of biological chemistry 20060317
Deregulation of cyclin-dependent kinase 2 activity correlates with UVC-induced apoptosis in Chinese hamster ovary cells. Journal of cellular biochemistry 20060301
Activities of maturation-promoting factor (MPF) and mitogen-activated protein kinase (MAPK) are not required for the global histone deacetylation observed after germinal vesicle breakdown (GVBD) in porcine oocytes. Reproduction (Cambridge, England) 20060301
Selectivity and potency of cyclin-dependent kinase inhibitors. The AAPS journal 20060301
Dual action of the inhibitors of cyclin-dependent kinases: targeting of the cell-cycle progression and activation of wild-type p53 protein. Expert opinion on investigational drugs 20060101
Potential use of pharmacological cyclin-dependent kinase inhibitors as anti-HIV therapeutics. Current pharmaceutical design 20060101
NORs and their transcription competence during the cell cycle. Folia biologica 20060101
Activation of CYP1A1 gene expression during primary culture of mouse hepatocytes. Toxicology 20051215
Indirubin-3'-monoxime, a derivative of a Chinese antileukemia medicine, inhibits P-TEFb function and HIV-1 replication. AIDS (London, England) 20051202
Molecular models of protein kinase 6 from Plasmodium falciparum. Journal of molecular modeling 20051201
Rapamycin worsens renal function and intratubular cast formation in protein overload nephropathy. Kidney international 20051201
[New strategy for the treatment of multiple myeloma]. [Rinsho ketsueki] The Japanese journal of clinical hematology 20051201
Roscovitine modulates DNA repair and senescence: implications for combination chemotherapy. Clinical cancer research : an official journal of the American Association for Cancer Research 20051115
Caspase 8/10 are not mediating apoptosis in neuroblastoma cells treated with CDK inhibitory drugs. European journal of pharmacology 20051107
A {gamma}-secretase-independent mechanism of signal transduction by the amyloid precursor protein. The Journal of biological chemistry 20051104
Roscovitine triggers excitotoxicity in cultured granule neurons by enhancing glutamate release. Molecular pharmacology 20051101
Potentiation of the lethality of the histone deacetylase inhibitor LAQ824 by the cyclin-dependent kinase inhibitor roscovitine in human leukemia cells. Molecular cancer therapeutics 20051101
Roscovitine is an effective inducer of apoptosis of Ewing's sarcoma family tumor cells in vitro and in vivo. Cancer research 20051015
Vitrification of calf oocytes: effects of maturation stage and prematuration treatment on the nuclear and cytoskeletal components of oocytes and their subsequent development. Molecular reproduction and development 20051001
Cyclin A2-CDK2 regulates embryonic gene activation in 1-cell mouse embryos. Developmental biology 20051001
Overexpression of regucalcin suppresses cell proliferation of cloned normal rat kidney proximal tubular epithelial NRK52E cells. International journal of molecular medicine 20051001
Roscovitine targets, protein kinases and pyridoxal kinase. The Journal of biological chemistry 20050902
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. The Journal of biological chemistry 20050902
Slowed N-type calcium channel (CaV2.2) deactivation by the cyclin-dependent kinase inhibitor roscovitine. Biophysical journal 20050901
Role of the cell cycle in the pathobiology of central nervous system trauma. Cell cycle (Georgetown, Tex.) 20050901
Accumulation of p53 and reductions in XIAP abundance promote the apoptosis of prostate cancer cells. Cancer research 20050901
Varicella-zoster virus IE63 protein phosphorylation by roscovitine-sensitive cyclin-dependent kinases modulates its cellular localization and activity. The Journal of biological chemistry 20050812
Seliciclib (CYC202 or R-roscovitine), a small-molecule cyclin-dependent kinase inhibitor, mediates activity via down-regulation of Mcl-1 in multiple myeloma. Blood 20050801
Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor. Cellular and molecular life sciences : CMLS 20050801
Inhibiting MAP kinase activity prevents calcium transients and mitosis entry in early sea urchin embryos. The Journal of biological chemistry 20050701
In vitro activity of cyclin-dependent kinase inhibitor CYC202 (Seliciclib, R-roscovitine) in mantle cell lymphomas. Annals of oncology : official journal of the European Society for Medical Oncology 20050701
Cdc2-mediated inhibition of epidermal growth factor activation of the extracellular signal-regulated kinase pathway during mitosis. The Journal of biological chemistry 20050701
In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202. Clinical cancer research : an official journal of the American Association for Cancer Research 20050701
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1. Cancer research 20050615
A novel CDK inhibitor, CYC202 (R-roscovitine), overcomes the defect in p53-dependent apoptosis in B-CLL by down-regulation of genes involved in transcription regulation and survival. Blood 20050601
Birth of piglets after transferring of in vitro-produced embryos pre-matured with R-roscovitine. Reproduction (Cambridge, England) 20050601
Implication of cyclin-dependent kinase 5 in the development of psychological dependence on and behavioral sensitization to morphine. Journal of neurochemistry 20050601
Neurotransmitter acetylcholine negatively regulates neuromuscular synapse formation by a Cdk5-dependent mechanism. Neuron 20050519
Cyclin-dependent kinase 5 mediates neurotoxin-induced degradation of the transcription factor myocyte enhancer factor 2. The Journal of neuroscience : the official journal of the Society for Neuroscience 20050511
Drugging cell cycle kinases in cancer therapy. Current drug targets 20050501
Neurotoxic calcium transfer from endoplasmic reticulum to mitochondria is regulated by cyclin-dependent kinase 5-dependent phosphorylation of tau. The Journal of neuroscience : the official journal of the Society for Neuroscience 20050420
c-Jun NH2-terminal kinase-interacting protein-3 facilitates phosphorylation and controls localization of amyloid-beta precursor protein. The Journal of neuroscience : the official journal of the Society for Neuroscience 20050413
Recent progress in the discovery and development of cyclin-dependent kinase inhibitors. Expert opinion on investigational drugs 20050401
Development and validation of a liquid chromatography and tandem mass spectrometry method for determination of roscovitine in plasma and urine samples utilizing on-line sample preparation. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20050325
p25/Cdk5-mediated retinoblastoma phosphorylation is an early event in neuronal cell death. Journal of cell science 20050315
Limitation of podocyte proliferation improves renal function in experimental crescentic glomerulonephritis. Kidney international 20050301
A small molecule-kinase interaction map for clinical kinase inhibitors. Nature biotechnology 20050301
Mechanism of CDK5/p25 binding by CDK inhibitors. Journal of medicinal chemistry 20050210
Mycophenolate mofetil and roscovitine decrease cyclin expression and increase p27(kip1) expression in anti Thy1 mesangial proliferative nephritis. Clinical and experimental immunology 20050201
Contribution of high p34cdc2 kinase activity to premature chromosome condensation of injected somatic cell nuclei in rat oocytes. Reproduction (Cambridge, England) 20050201
Cdk inhibition in human cells compromises chk1 function and activates a DNA damage response. Cancer research 20050201
Antiviral activity of CYC202 in HIV-1-infected cells. The Journal of biological chemistry 20050128
Maintenance of meiotic arrest in bovine oocytes using the S-enantiomer of roscovitine: effects on maturation, fertilization and subsequent embryo development in vitro. Reproduction (Cambridge, England) 20050101
Roscovitine-induced up-regulation of p53AIP1 protein precedes the onset of apoptosis in human MCF-7 breast cancer cells. Molecular cancer therapeutics 20050101
Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-roscovitine in the mouse. Molecular cancer therapeutics 20050101
Intrathecal administration of roscovitine inhibits Cdk5 activity and attenuates formalin-induced nociceptive response in rats. Acta pharmacologica Sinica 20050101
Blockage of cyclin cdk's, PKC and phosphoinositol 3-kinase pathways leads to augmentation of apoptosis in drug-resistant leukemia cells: evidence for interactive effects of flavopiridol, LY 294002, roscovitine,wortmannin and UCN-01. Anticancer research 20050101
Role of cyclin-dependent kinase 5 and its activator P35 in local axon and growth cone stabilization. Neuroscience 20050101
Cdk inhibitory nucleoside analogs prevent transcription from viral genomes. Nucleosides, nucleotides & nucleic acids 20050101
GTP-dependent secretion from neutrophils is regulated by Cdk5. The Journal of biological chemistry 20041224
A major role for mitotic CDC2 kinase inactivation in the establishment of the mitotic DNA damage checkpoint. Cancer research 20041215
Regulation of cyclin-dependent kinase 5 and calcium/calmodulin-dependent protein kinase II by phosphatidylinositol-linked dopamine receptor in rat brain. Molecular pharmacology 20041201
Programmed cell death protein 4 suppresses CDK1/cdc2 via induction of p21(Waf1/Cip1). American journal of physiology. Cell physiology 20041201
Several signaling pathways are involved in the control of cattle oocyte maturation. Molecular reproduction and development 20041201
Characterization of a novel ATR-dependent, Chk1-independent, intra-S-phase checkpoint that suppresses initiation of replication in Xenopus. Journal of cell science 20041201
E2F4 deficiency promotes drug-induced apoptosis. Cancer biology & therapy 20041201
Molecular models of cyclin-dependent kinase 1 complexed with inhibitors. Biochemical and biophysical research communications 20041112
Transition of G1 to early S phase may be required for zinnia mesophyll cells to trans-differentiate to tracheary elements. Planta 20041101
Proteasomes act in the pre-mitochondrial signal transduction route towards roscovitine-induced apoptosis. International journal of oncology 20041101
Endogenous regulators of protein phosphatase-1 during mouse oocyte development and meiosis. Reproduction (Cambridge, England) 20041101
Repression of G0/G1 traverse in human fibroblasts exposed to low levels of ionizing radiation. The Journal of biological chemistry 20041015
Regulation of histone acetylation during meiotic maturation in mouse oocytes. Molecular reproduction and development 20041001
Identification of tyrosine hydroxylase as a physiological substrate for Cdk5. Journal of neurochemistry 20041001
Glycogen synthase kinase-3 inhibitors prevent caspase-dependent apoptosis induced by ethanol in cultured rat cortical neurons. European journal of pharmacology 20040924
Effect of prematuration, meiosis activating sterol and enriched maturation medium on the nuclear maturation and competence to development of calf oocytes. Theriogenology 20040915
Retinoid-dependent mRNA expression and poly-(A) contents in bovine oocytes meiotically arrested and/or matured in vitro. Molecular reproduction and development 20040901
Cyclin-dependent kinase inhibitors attenuate protein hyperphosphorylation, cytoskeletal lesion formation, and motor defects in Niemann-Pick Type C mice. The American journal of pathology 20040901
P21Cip1 is a critical mediator of the cytotoxic action of thymidylate synthase inhibitors in colorectal carcinoma cells. Cancer research 20040901
Intrathecal cdk5 inhibitor, roscovitine, attenuates morphine antinociceptive tolerance in rats. Acta pharmacologica Sinica 20040801
Meiotic inhibition with different cyclin-dependent kinase inhibitors in bovine oocytes and its effects on maturation and embryo development. Zygote (Cambridge, England) 20040801
Involvement of Cdk5/p25 in digoxin-triggered prostate cancer cell apoptosis. The Journal of biological chemistry 20040709
The retinoic acid and brain-derived neurotrophic factor differentiated SH-SY5Y cell line as a model for Alzheimer's disease-like tau phosphorylation. Biochemical and biophysical research communications 20040702
Transient cerebral ischemia induces aberrant neuronal cell cycle re-entry and Alzheimer's disease-like tauopathy in female rats. The Journal of biological chemistry 20040521
The human nuclear SRcyp is a cell cycle-regulated cyclophilin. The Journal of biological chemistry 20040521
Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons. Biochemical pharmacology 20040515
Analysis of CDK2 active-site hydration: a method to design new inhibitors. Proteins 20040501
Cell differentiation, caspase inhibition, and macromolecular synthesis blockage, but not BCL-2 or BCL-XL proteins, protect SH-SY5Y cells from apoptosis triggered by two CDK inhibitory drugs. Experimental cell research 20040415
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. Bioorganic & medicinal chemistry letters 20040405
TBP-associated factor 1 overexpression induces tolerance to Doxorubicin in confluent H9c2 cells by an increase in cdk2 activity and cyclin E expression. Molecular and cellular biochemistry 20040401
Regulation of binding of lamin B receptor to chromatin by SR protein kinase and cdc2 kinase in Xenopus egg extracts. The Journal of biological chemistry 20040326
Role of p300 and PCAF in regulating cyclooxygenase-2 promoter activation by inflammatory mediators. Blood 20040315
Viral and cellular kinases are potential antiviral targets and have a central role in varicella zoster virus pathogenesis. Biochimica et biophysica acta 20040311
Enhanced sensitivity to irinotecan by Cdk1 inhibition in the p53-deficient HT29 human colon cancer cell line. Oncogene 20040304
Antiapoptotic effects of roscovitine in cerebellar granule cells deprived of serum and potassium: a cell cycle-related mechanism. Neurochemistry international 20040301
Roscovitine, a cyclin-dependent kinase inhibitor, prevents replication of varicella-zoster virus. Journal of virology 20040301
Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis. Molecular cancer therapeutics 20040301
Analysis of roscovitine using novel high performance liquid chromatography and UV-detection method: pharmacokinetics of roscovitine in rat. Journal of pharmaceutical and biomedical analysis 20040204
Protection of renal cells from cisplatin toxicity by cell cycle inhibitors. American journal of physiology. Renal physiology 20040201
Angiostatin-induced inhibition of endothelial cell proliferation/apoptosis is associated with the down-regulation of cell cycle regulatory protein cdk5. Journal of cellular biochemistry 20040201
Cdk5 phosphorylation of doublecortin ser297 regulates its effect on neuronal migration. Neuron 20040122
Potent, selective and cell-mediated inhibition of human herpesvirus 6 at an early stage of viral replication by the non-nucleoside compound CMV423. Biochemical pharmacology 20040115
The development of a CDK2-docking site peptide that inhibits p53 and sensitizes cells to death. Cell cycle (Georgetown, Tex.) 20040101
A novel approach to develop anti-HIV drugs: adapting non-nucleoside anticancer chemotherapeutics. Antiviral research 20040101
The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway. Cancer research 20040101
[Antiproliferative effect of bcl-2 gene does not concern the control of mitotic events]. Tsitologiia 20040101
Mechanism of sulforaphane-induced cell cycle arrest and apoptosis in human colon cancer cells. Nutrition and cancer 20040101
Expression profiles of a human pancreatic cancer cell line upon induction of apoptosis search for modulators in cancer therapy. Oncology 20040101
Cell cycle arrest induced in human breast cancer cells by cyclin-dependent kinase inhibitors: a comparison of the effects exerted by roscovitine and olomoucine. Polish journal of pharmacology 20040101
Divergent roles of GSK3 and CDK5 in APP processing. Biochemical and biophysical research communications 20031226
The expression of retinoblastoma and Sp1 is increased by low concentrations of cyclin-dependent kinase inhibitors. European journal of biochemistry 20031201
Roscovitine inhibits STAT5 activity and induces apoptosis in the human leukemia virus type 1-transformed cell line MT-2. Cancer research 20031201
The M-phase-promoting factor modulates the sensitivity of the Ca2+ stores to inositol 1,4,5-trisphosphate via the actin cytoskeleton. The Journal of biological chemistry 20031024
Chemical inhibitors of cyclin-dependent kinases control proliferation, apoptosis and differentiation of oligodendroglial cells. International journal of developmental neuroscience : the official journal of the International Society for Developmental Neuroscience 20031001
Effect of cycloheximide, 6-DMAP, roscovitine and butyrolactone I on resumption of meiosis in porcine oocytes. Theriogenology 20031001
Neuroprotective action of flavopiridol, a cyclin-dependent kinase inhibitor, in colchicine-induced apoptosis. Neuropharmacology 20031001
Cdk2-dependent phosphorylation of the NF-Y transcription factor and its involvement in the p53-p21 signaling pathway. The Journal of biological chemistry 20030919
2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors. Bioorganic & medicinal chemistry letters 20030915
High-throughput screening for the identification of small-molecule inhibitors of retinoblastoma protein phosphorylation in cells. Analytical biochemistry 20030901
Effects of meiosis-inhibiting agents and equine chorionic gonadotropin on nuclear maturation of canine oocytes. Molecular reproduction and development 20030801
Cdk5 is essential for synaptic vesicle endocytosis. Nature cell biology 20030801
Antiapoptotic and protective effects of roscovitine on ischemia-reperfusion injury of the rat liver. Liver international : official journal of the International Association for the Study of the Liver 20030801
Cell cycle-dependent phosphorylation of Disabled-2 by cdc2. Oncogene 20030717
Mitotic and stress-induced phosphorylation of HsPI3K-C2alpha targets the protein for degradation. The Journal of biological chemistry 20030711
Endoplasmic reticulum reorganizations and Ca2+ signaling in maturing and fertilized oocytes of marine protostome worms: the roles of MAPKs and MPF. Development (Cambridge, England) 20030701
Regulation of ania-6 splice variants by distinct signaling pathways in striatal neurons. Journal of neurochemistry 20030701
The effect of roscovitine on herpetic keratitis. Experimental eye research 20030601
Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials. Accounts of chemical research 20030601
Signaling through Cdk2, importin-alpha and NuMA is required for H2O2-induced mitosis in primary type II pneumocytes. Biochimica et biophysica acta 20030512
Specific inhibition of mouse oocyte nuclear protein phosphatase-1 stimulates germinal vesicle breakdown. Molecular reproduction and development 20030501
Synthesis and biological evaluations of pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 inhibitors. European journal of medicinal chemistry 20030501
The lethal effects of pharmacological cyclin-dependent kinase inhibitors in human leukemia cells proceed through a phosphatidylinositol 3-kinase/Akt-dependent process. Cancer research 20030415
The specificities of protein kinase inhibitors: an update. The Biochemical journal 20030401
Ultrastructural modifications in bovine oocytes maintained in meiotic arrest in vitro using roscovitine or butyrolactone. Molecular reproduction and development 20030301
Cyclin-dependent kinase inhibitor, roscovitine, in combination with exogenous cytokinin, N6-benzyladenine, causes increase of cis-cytokinins in immobilized tobacco cells. Biotechnology letters 20030301
Cocaine-induced proliferation of dendritic spines in nucleus accumbens is dependent on the activity of cyclin-dependent kinase-5. Neuroscience 20030101
Inhibitors of diverse metabolic steps cause increased apoptosis in deoxyadenosine-resistant mouse leukemia L1210 cells that lack p53 expression: convergence at caspase-3 activation. Advances in enzyme regulation 20030101
Human cytomegalovirus (HCMV) IE1 plays role in resistance to apoptosis with etoposide in cancer cell line by Cdk2 accumulation. Microbiology and immunology 20030101
Synthesis and biological activity of olomoucine II. Bioorganic & medicinal chemistry letters 20021118
Influence of phosphorylation of p35, an activator of cyclin-dependent kinase 5 (cdk5), on the proteolysis of p35. Brain research. Molecular brain research 20021015
Molecular model of cyclin-dependent kinase 5 complexed with roscovitine. Biochemical and biophysical research communications 20021011
Human p14(Arf): an exquisite sensor of morphological changes and of short-lived perturbations in cell cycle and in nucleolar function. Oncogene 20021003
Dynamics and binding modes of free cdk2 and its two complexes with inhibitors studied by computer simulations. Journal of biomolecular structure & dynamics 20021001
Protective effect of roscovitine on renal ischemia-reperfusion injury. Transplantation proceedings 20020901
Pharmacological cyclin-dependent kinase inhibitors inhibit replication of wild-type and drug-resistant strains of herpes simplex virus and human immunodeficiency virus type 1 by targeting cellular, not viral, proteins. Journal of virology 20020801
Embryonic and foetal development of bovine oocytes treated with a combination of butyrolactone I and roscovitine in an enriched medium prior to IVM and IVF. Molecular reproduction and development 20020801
Inhibition of cyclin-dependent kinase 1 by purines and pyrrolo[2,3-d]pyrimidines does not correlate with antiviral activity. Antimicrobial agents and chemotherapy 20020801
Modifications of the Ca2+ release mechanisms of mouse oocytes by fertilization and by sperm factor. Molecular human reproduction 20020701
Roscovitine inhibits ongoing DNA synthesis in human cervical cancer. Cancer letters 20020606
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes. Journal of medicinal chemistry 20020606
Roscovitine: a novel regulator of P/Q-type calcium channels and transmitter release in central neurons. The Journal of physiology 20020501
Beta-carbolines as specific inhibitors of cyclin-dependent kinases. Bioorganic & medicinal chemistry letters 20020408
Cdk5/p35 regulates neurotransmitter release through phosphorylation and downregulation of P/Q-type voltage-dependent calcium channel activity. The Journal of neuroscience : the official journal of the Society for Neuroscience 20020401
Adenovirus-mediated E2F-1 gene transfer sensitizes melanoma cells to apoptosis induced by topoisomerase II inhibitors. Cancer research 20020315
Modulation of intrinsic P-glycoprotein expression in multicellular prostate tumor spheroids by cell cycle inhibitors. Biochimica et biophysica acta 20020213
Mitosis-dependent phosphorylation and activation of LIM-kinase 1. Biochemical and biophysical research communications 20020201
cAMP-Dependent PKA negatively regulates polyadenylation of c-mos mRNA in rat oocytes. Molecular endocrinology (Baltimore, Md.) 20020201
Suppression of meiosis by inhibitors of m-phase proteins in horse oocytes with low meiotic competence. Zygote (Cambridge, England) 20020201
Evidence for a pre-restriction point Cdk3 activity. Journal of cellular biochemistry 20020101
E2F-1 gene therapy induces apoptosis and increases chemosensitivity in human pancreatic carcinoma cells. Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine 20020101
When cell biology and neurobiology meet. Genome biology 20020101
Suppression of HIV-1 expression by inhibitors of cyclin-dependent kinases promotes differentiation of infected podocytes. Journal of the American Society of Nephrology : JASN 20011201
Bovine oocytes treated prior to in vitro maturation with a combination of butyrolactone I and roscovitine at low doses maintain a normal developmental capacity. Molecular reproduction and development 20011201
The cyclin-dependent kinase inhibitor roscovitine inhibits RNA synthesis and triggers nuclear accumulation of p53 that is unmodified at Ser15 and Lys382. Molecular pharmacology 20011001
The neuropeptide head activator induces activation and translocation of the growth-factor-regulated Ca(2+)-permeable channel GRC. Journal of cell science 20011001
Common and reversible regulation of wild-type p53 function and of ribosomal biogenesis by protein kinases in human cells. Oncogene 20010920
Cyclin-dependent kinase 5 promotes insulin exocytosis. The Journal of biological chemistry 20010907
Structure-activity relationships and inhibitory effects of various purine derivatives on the in vitro growth of Plasmodium falciparum. Biochemical pharmacology 20010801
Inhibition of human immunodeficiency virus type 1 transcription by chemical cyclin-dependent kinase inhibitors. Journal of virology 20010801
Nuclear ultrastructure in bovine oocytes after inhibition of meiosis by chemical and biological inhibitors. Molecular reproduction and development 20010801
Activation of p53 by roscovitine-mediated suppression of MDM2 expression. Oncogene 20010531
5-HT causes an increase in cAMP that stimulates, rather than inhibits, oocyte maturation in marine nemertean worms. Development (Cambridge, England) 20010401
Evidence that Fas-induced apoptosis leads to S phase arrest. Human immunology 20010401
Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species. Journal of natural products 20010401
Effects of chronic exposure to cocaine are regulated by the neuronal protein Cdk5. Nature 20010315
Caspase-mediated Cdk2 activation is a critical step to execute transforming growth factor-beta1-induced apoptosis in human gastric cancer cells. Oncogene 20010308
Stoichiometric phosphorylation of human p53 at Ser315 stimulates p53-dependent transcription. The Journal of biological chemistry 20010216
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717. Journal of medicinal chemistry 20010215
The relationship between differentiation and survival in PC12 cells treated with cyclic adenosine monophosphate in the presence of epidermal growth factor or nerve growth factor. Neuroscience letters 20010112
Regulation of thymidine kinase expression during cellular senescence. Journal of biomedical science 20010101
Augmentation of apoptosis responses in p53-deficient L1210 cells by compounds directed at blocking NFkappaB activation. Anticancer research 20010101
Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase. Antiviral research 20001001
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorganic & medicinal chemistry letters 20000306
Phosphorylation of steroidogenic factor 1 is mediated by cyclin-dependent kinase 7. Molecular endocrinology (Baltimore, Md.)

© 2019 Angene International Limited. All rights Reserved.