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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> CDK

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. GC36312 Indirubin-3'-monoxime-5-sulphonic acid Indirubin-3'-monoxime-5-sulphonic acid 是一种有效选择性的 CDK1，CDK5，GSK-3β 抑制剂，对应的 IC50 值分别为 5 nM，7 nM，80 nM。
  3. GC36062 FMF-04-159-2 FMF-04-159-2 是一种有效的共价 CDK14 抑制剂。FMF-04-159-2 抑制 CDK14 和 CDK2，在 NanoBRET 试验中 IC50 分别为 39.6 nM 和 256 nM。
  4. GC35739 CP-10 CP-10 是具有高选择性，特异性和显著的 CDK6 降解潜力 (DC50=2.1 nM) 的 PROTAC。它抑制几种造血细胞癌的增殖，包括多发性骨髓瘤，并且对突变和过表达的 CDK6 仍然可以降解。
  5. GC35636 CDK9-IN-7 CDK9-IN-7 (compound 21e) 是一种高效选择性的，具有口服活性的 CDK9/cyclin T 抑制剂 (IC50=11 nM)，与抑制其他 CDK 相比更有效 (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM)。CDK9-IN-7 具有抗癌活性并没有明显的毒性。CDK9-IN-7 诱导非小细胞肺癌 (NSCLC) 细胞凋亡，在 G2 期阻滞细胞周期，并具有抑制非小细胞肺癌干度的特性。
  6. GC35635 CDK9 Antagonist-1 CDK9 Antagonist-1 是一种基于 PROTAC 技术，高效选择性的 CDK9 降解剂，在 MCF-7 细胞系中抑制 CDK9 的 IC50 值为 17 μM。PROTAC 由天然产物汉黄芩素 (Wogonin) 与泛素 E3 连接酶 (CRBN) 通过 linker 连接而成。
  7. GC35634 CDK4/6-IN-3 CDK4/6-IN-3 是一种脑渗透性的 CDK4/CDK6 抑制剂，Ki 分别为 <0.3 nM 和 2.2 nM。CDK4/6-IN-3 抑制 CDK1，Ki 为 110 nM。CDK4/6-IN-3 可用于治疗胶质母细胞瘤。
  8. GC35633 CDK4/6-IN-2 CDK4/6-IN-2 是一种有效的 CDK4 和 CDK6 抑制剂，IC50 分别为 2.7 和 16 nM，详细信息请参考专利文献 US20180000819A1 中 的化合物 1。
  9. GC35632 CDK2-IN-4 CDK2-IN-73 (CDK2-IN-4, CDK2 inhibitor 73) is a potent and selective inhibitor of CDK2 with IC50 of 44 nM for CDK2/cyclin A.
  10. GC35628 Cdc7-IN-1 Cdc7-IN-1 (Compound 13) 是一种高效、选择性的 ATP 竞争性的 Cdc7 激酶抑制剂，在 1 mM ATP 存在时对 Cdc7 作用的 IC50 值为 0.6 nM，具有解离率低的特质。Cdc7-IN-1 能高效地抑制癌细胞中的 Cdc7，诱导细胞死亡。
  11. GC35512 BI-1347 BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM.
  12. GC35315 AMG 925 HCl A dual inhibitor of FLT3 and Cdk4
  13. GC35218 Abemaciclib Metabolites M2

    LSN2839567

     Abemaciclib Metabolites M2 (LSN2839567) 是 Abemaciclib 的代谢物，是一种有效的 CDK4 和 CDK6 抑制剂，IC50 分别为 1.2 和 1.3 nM。抗癌活性。
  14. GC35162 5-Iodo-indirubin-3'-monoxime 5-Iodo-indirubin-3'-monoxime 是一种有效的 GSK-3β，CDK5/P25 和 CDK1/cyclin B 抑制剂，与 ATP 竞争性地结合酶的催化位点，IC50 值分别为 9，20 和 25 nM。
  15. GC35022 [pThr3]-CDK5 Substrate [pThr3]-CDK5 Substrate 是有效的 Thr3 位点磷酸化的 CDK5 底物。[pThr3]-CDK5 Substrate 衍生自组蛋白 H1 肽序列，位于 CDK5 的活性位点。[pThr3]-CDK5 Substrate 被 CDK5 磷酸化，Km 为 6 μM。
  16. GC35021 [pSer2, pSer5, pSer7]-CTD TFA [pSer2, pSer5, pSer7]-CTD (TFA) 是 CDK7 的一个底物，是 RNA 聚合酶 II 羧基端域 (CTD) 的 ser2、ser5 和 ser7 位点磷酸化的多肽。
  17. GC43175 CAY10574 A Cdk2-cyclin E and Cdk9 inhibitor
  18. GC41716 (R)-CR8

    (2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8, (R)-Isomer

     An inhibitor of cyclin-dependent kinases
  19. GC34692 NU6140 A Cdk2 inhibitor
  20. GC34650 Longdaysin

    Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7.
  21. GC40092 PD 0332991-d8

    帕博西尼-D8,PD 0332991-d8

     An internal standard for the quantification of PD 0332991
  22. GC34422 Atuveciclib (BAY-1143572) Atuveciclib(BAY-1143572)是一种口服有效的高选择性PTEFb/CDK9抑制剂。Atuveciclib(BAY-1143572)抑制CDK9/CycT1，IC50为13nM。
  23. GC34421 Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) AtuveciclibS-Enantiomer(BAY-1143572S-Enantiomer)是一种有效的选择性CDK9抑制剂，抑制CDK9/CycT1，IC50为16nM。
  24. GC34355 SEL120-34A monohydrochloride A dual inhibitor of Cdk8 and Cdk19
  25. GC34204 JSH-150 JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
  26. GC34163 Lerociclib (G1T38)

    G1T38

     G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.
  27. GC34124 (rel)-MC180295

    (rel)-MC180295

     MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.
  28. GC34118 Trilaciclib (G1T28)

    曲拉西利,G1T28

     Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively.
  29. GC34100 Lerociclib dihydrochloride (G1T38 dihydrochloride)

    G1T38 dihydrochloride

     Lerociclib dihydrochloride (G1T38 dihydrochloride) (G1T38 dihydrochloride) 是一种有效的选择性 CDK4/CDK6 抑制剂，对 CDK4/CyclinD1 和 CDK6/CyclinD3 的 IC50 分别为 1 nM 和 2 nM。
  30. GC34087 Trilaciclib hydrochloride (G1T28 hydrochloride)

    曲拉西利双盐酸盐,G1T28 hydrochloride

     Trilaciclib hydrochloride (G1T28 hydrochloride) (G1T28 hydrochloride) 是一种 CDK4/6 抑制剂，对 CDK4 和 CDK6 的 IC50 分别为 1 nM 和 4 nM。
  31. GC34059 Atuveciclib Racemate (BAY-1143572 Racemate)

    BAY-1143572 Racemate

     Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
  32. GC34056 NVP-2 A Cdk9/cyclin T1 complex inhibitor
  33. GC33366 CDK8-IN-4 CDK8-IN-4是CDK8的抑制剂，来自专利WO2014090692A1,化合物实例16,IC50值为0.2nM。
  34. GC33360 Roniciclib (BAY 1000394)

    BAY 1000394

     Roniciclib (BAY 1000394) 是一种可口服的泛细胞周期蛋白依赖性激酶 (CDK) 抑制剂，对 CDK1、CDK2、CDK3、CDK4、CDK7 和 CDK9 的 IC50 为 5-25 nM。
  35. GC33353 ON-013100 ON-013100，一种抗肿瘤药物，作为有丝分裂的抑制剂，能够抑制细胞周期蛋白D1(CyclinD1)的表达。
  36. GC33327 CMPD 7 CMPD 7 是一种有效的选择性 CDK12 抑制剂，在酶促试验中的 IC50 为 491 nM。
  37. GC33180 CDK8-IN-1 CDK8-IN-1是一个有效的、CDK8的选择性抑制剂，其IC50值为3nM。
  38. GC33137 SEL120-34A A dual inhibitor of Cdk8 and Cdk19
  39. GC33107 (±)-BAY-1251152

    (±)-BAY-1251152; (±)-VIP152

     A racemic mixture of (+)-BAY-1251152 and (–)-BAY-1251152
  40. GC33049 FN-1501 FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.
  41. GC32970 MBQ-167

    MBQ-167是Ras相关的C3型肉毒素底物(Rac)和细胞分裂周期蛋白(Cdc42)的双抑制剂，其对Rac1/2/3的IC50值为103nM，对Cdc42的IC50值为78nM。
  42. GC32930 Simurosertib (TAK-931)

    TAK-931

     An inhibitor of Cdc7 kinase
  43. GC32898 SEL120-34A HCl A dual inhibitor of Cdk8 and Cdk19
  44. GC32845 PROTAC CDK9 Degrader-1

    N-(5-环丁基-1H-吡唑-3-基)-2-(4-((5-((2-(2,6-二氧代哌啶-3-基)-1,3-二氧代异吲哚啉-4-基)氧基)戊基)氧基)苯基)乙酰胺

     PROTACCDK9Degrader-1是一种有选择性的CDK9降解剂。
  45. GC32832 PF-06873600

    PF-3600

     An inhibitor of Cdk2, Cdk4, and Cdk6
  46. GC32829 NU6300 NU6300是一种共价的ATP竞争性CDK2抑制剂。
  47. GC32746 MSC2530818 A Cdk8 inhibitor
  48. GC32741 CCT-251921 CCT-251921是有效，选择性，有口服活性的CDK8抑制剂；IC50值为2.3nM。
  49. GC32735 Samuraciclib hydrochloride (ICEC0942 hydrochloride)

    CT7001 hydrochloride; ICEC0942 hydrochloride

     Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.
  50. GC32717 AZD4573 AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.
  51. GC32700 CYC065

    CYC065

     An inhibitor of Cdk2 and Cdk9

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