Roscovitine (R)-2-((6-(苄基氨基)-9-异丙基-9H-嘌呤-2-基)氨基)丁-1-醇
CAS 186692-46-6 MFCD02266401
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资金保障
专业采购外包团队在线服务
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分类
- {SA} A to C, Antitumor Agents, Apoptosis and Cell Cycle, Bioactive Small Molecules, Biochemicals and Reagents, Cancer Research, Cell Biology, Cell Cycle Proteins and Antibodies, Cell Cycle Regulators, Cell Signaling and Neuroscience, Cyclin Dependent Kinases, Cyclin-Dependent Kinase (CDK), Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, Kinase/Phosphatase Biology, R, Serine/Threonine Kinase Biology, Serine/Threonine Kinase Inhibitors
- {SNA} A to C, Antitumor Agents, Apoptosis and Cell Cycle, Bioactive Small Molecules, Biochemicals and Reagents,
- {SNA} A to C,
产品应用
- Seliciclib, also known as roscovitine and CYC202, is a n orally bioavailable, small-molecule cyclin-dependent kinase (CDK) inhibitor with potential proapoptotic and antineoplastic activities. Seliciclib primarily inhibits CDK2/E, CDK2/A, CDK7 and CDK9 by competing for their ATP binding sites, leading to a disruption of cell cycle progression. In addition, this agent appears to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, inhibiting RNA polymerase II-dependent transcription, which may result in the down-regulation of antiapoptotic proteins such as induced myeloid leukemia cell differentiation protein Mcl-1.
相关文献及参考
- DeAzevado, W.F., et al., Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine. Eur. J. Biochem. 243 , 518-526, (1997) 摘要
- Chen, M.C., et al., Involvement Of CAMP In Nerve Growth Factor-triggered P35/Cdk5 Activation And Differentiation In PC12 Cells. Am. J. Physiol. Cell Physiol. 299 , C516-27, (2010) 摘要
- Merck 14 ,10240
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