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CDK(细胞周期蛋白依赖性激酶)

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.

There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.

CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).

Products for  CDK

  1. Cat.No. 产品名称 Information
  2. GC10842 LEE011 A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor
  3. GC16425 Flavopiridol hydrochloride An inhibitor of cyclin-dependent kinases
  4. GC16268 Purvalanol B A CDK inhibitor
  5. GC17648 Dinaciclib(SCH727965) A CDK inhibitor
  6. GC12865 BMS265246 A cell-permeable inhibitor of Cdk1 and Cdk2
  7. GC15588 PHA-848125 An inhibitor of Cdks
  8. GC15421 Palbociclib (PD0332991) Isethionate Palbociclib (PD 0332991) isethionate 是一种具有口服活性的选择性 CDK4 和 CDK6 抑制剂,IC50 值分别为 11 和 16 nM。 Palbociclib (PD0332991) Isethionate 具有有效的抗增殖活性,可诱导癌细胞的细胞周期停滞,可用于 HR 阳性和 HER2 阴性乳腺癌和肝细胞癌的研究。
  9. GC12438 AZD-5438 A potent inhibitor of CDKs
  10. GC17935 PD 0332991 (Palbociclib) HCl A selective cyclin D kinase 4/6 inhibitor
  11. GC16822 LY2835219 A dual inhibitor of CDK4 and CDK6
  12. GC15870 AT7519 A Cdk inhibitor
  13. GC13690 BS-181 HCl A selective Cdk7 inhibitor
  14. GC15047 PHA-793887 A CDK inhibitor
  15. GC11401 Roscovitine (Seliciclib,CYC202) A potent inhibitor of cyclin-dependent kinase 2
  16. GC11396 SNS-032 (BMS-387032) A Cdk2, Cdk7, and Cdk9 inhibitor
  17. GC15571 SU 9516 A pro-apoptotic Cdk2/cyclin A inhibitor
  18. GC12064 SB1317 A multi-kinase inhibitor
  19. GC11324 PHA-767491 A potent Cdc7 kinase inhibitor
  20. GC16959 NVP-LCQ195 NVP-LCQ195 (AT9311; LCQ195) 是 CDK1、CDK2、CDK3 和 CDK5 的小分子杂环抑制剂,IC50 为 1-42 nM。
  21. GC11823 LY2835219 free base A dual inhibitor of Cdk4 and Cdk6
  22. GC16063 Flavopiridol An inhibitor of cyclin-dependent kinases
  23. GC18028 CVT-313 A Cdk2 inhibitor
  24. GC17359 CDK9 inhibitor 2 CDK9 inhibitor 2 是一种特殊的细胞周期蛋白依赖性激酶 9 (CDK9) 抑制剂,提取自专利 WO/2012131594A1,化合物 CDKI(8),在 H929 多发性骨髓瘤 (MM) 细胞系中的 IC50 分别为 5 nM 和 7 nM(72 小时) ) 和 A2058 皮肤细胞系(72 小时)。
  25. GC12871 CDK9 inhibitor CDK9 inhibitor 是一种新型的选择性 CDK9 抑制剂,用于治疗 HIV 感染,对 CDK9/CycT1 的 IC50 为 39 nM,从参考化合物 87 中提取。
  26. GC12425 CDK inhibitor II CDK inhibitor II 是一种有效且特异性的 CDK9 抑制剂,IC50 <8 nM,取自参考文献 1,实施例 4。
  27. GC12001 BS-181 A selective Cdk7 inhibitor
  28. GC15597 AT7519 trifluoroacetate AT7519 (AT7519M) TFA 作为一种有效的 CDK 抑制剂,对 CDK1、CDK2、CDK4 到 CDK6 和 CDK9 的 IC50 分别为 210、47、100、13、170 和 <10 nM。
  29. GC13998 AT7519 Hydrochloride A Cdk inhibitor
  30. GC12612 JNJ-7706621 A dual inhibitor of CDKs and Aurora kinases
  31. GN10696 Garcinone C Garcinone C 是一种黄酮衍生物,是一种从 Garcinia oblongifolia Champ 中提取的天然化合物,用作抗炎、收敛和促进肉芽的药物,对某些癌症具有潜在的细胞毒性作用。 Garcinone C 刺激 ATR 和 4E-BP1 的表达水平,同时有效抑制 cyclin B1、cyclin D1、cyclin E2、cdc2、Stat3 和 CDK7 的表达水平。 Garcinone C 以时间和剂量依赖性方式显着抑制人鼻咽癌 (NPC) 细胞系 CNE1、CNE2、HK1 和 HONE1 的细胞活力。
  32. GN10526 Cucurbitacin E A natural triterpene
  33. GN10017 Wogonin A flavonoid with anti-inflammatory and antitumor activities

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