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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. GC62653 bio-THZ1 bio-THZ1 是THZ1 的生物素结构，与CDK7 不可逆的结合。THZ1 是有效，选择性的共价 CDK7 抑制剂，IC50 为 3.2 nM。
  3. GC62638 Ribociclib D6 hydrochloride

    LEE011-d6 hydrochloride

     Ribociclib D6 (LEE011 D6) hydrochloride 是 Ribociclib 的一种氘代化合物。Ribociclib 是一种高度特异性的 CDK4/6 抑制剂，IC50 值分别为 10 nM 和 39 nM，对 cyclin B/CDK1 复合体的活性低于其 1000 倍。
  4. GC62596 CDK7-IN-3

    7-(二甲基膦基)-3-[2-[[(3S)-6,6-二甲基-3-哌啶基]氨基]-5-(三氟甲基)-4-嘧啶基]-1H-吲哚-6-甲腈,CDK7-IN-3

     CDK7-IN-3 (CDK7-IN-3) 是一种具有口服活性的高选择性非共价 CDK7 抑制剂，KD 为 0.065 nM。 CDK7-IN-3 对 CDK2 (Ki=2600 nM)、CDK9 (Ki=960 nM)、CDK12 (Ki=870 nM) 显示出较差的抑制作用。 CDK7-IN-3 诱导肿瘤细胞凋亡并具有抗肿瘤活性。
  5. GC62572 hSMG-1 inhibitor 11e hSMG-1 inhibitor 11e 是一种有效的选择性的 hSMG-1 激酶抑制剂，其 IC50 值 <0.05 nM。hSMG-1 inhibitor 11e 对 hSMG-1 的选择性比 mTOR (IC50 为 45 nM)，PI3Kα/γ (IC50 为 61 nM 和 92 nM) 和 CDK1/CDK2 (IC50 为 32 μM 和 7.1 μM) 高 900 倍。
  6. GC62442 Casein Kinase inhibitor A51 Casein Kinase inhibitor A51 是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂。Casein Kinase inhibitor A51 可诱导白血病细胞凋亡 (apoptosis)，并具有有效的抗白血病活性。
  7. GC62427 Cdc7-IN-5 Cdc7-IN-5 (compound I-B) 是一种有效的 Cdc7 激酶抑制剂，详情请参考文献 WO2019165473A1，compound I-B。Cdc7 是一种丝氨酸苏氨酸蛋白激酶酶，在细胞周期中对 DNA 复制的启动至关重要。
  8. GC62423 GSK-3/CDK5/CDK2-IN-1 GSK-3/CDK5/CDK2-IN-1，一种咪唑衍生物，是 cdk5，cdk2 和 GSK-3 的抑制剂。GSK-3/CDK5/CDK2-IN-1 可用于癌症和神经退行性疾病的研究。详细信息请参考专利文献 WO2002010141A1 中的化合物 9a。
  9. GC62392 KB-0742 dihydrochloride KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.
  10. GC62319 Samuraciclib trihydrochloride Samuraciclib (CT7001) trihydrochloride 是一种有效的，具有选择性，ATP 竞争性和口服活性的 CDK7 抑制剂，IC50 为 41 nM。Samuraciclib trihydrochloride 对 CDK7 的选择性分别是 CDK1，CDK2 (IC50 为 578 nM)，CDK5 和 CDK9 的 45 倍，15 倍，230 倍和 30 倍。Samuraciclib trihydrochloride 以 GI50 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长，具有有效的抗肿瘤作用。
  11. GC62294 YKL-5-124 YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13.
  12. GC62263 BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.
  13. GC62168 CDK-IN-6

    (S)-2-(1-(3-乙基-7-((吡啶-3-基甲基)氨基)吡唑并[1,5-A]嘧啶-5-基)

     CDK-IN-6，是一类吡唑并[1,5-a]嘧啶化合物，是一种具有抗癌活性的 CDK 抑制剂。
  14. GC62139 XY028-140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).
  15. GC62112 Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
  16. GC61925 hSMG-1 inhibitor 11j

    嘧啶杂质1

     hSMG-1 inhibitor 11j，一种嘧啶衍生物，是有效的和选择性的 hSMG-1 抑制剂，IC50 值为 0.11 nM。hSMG-1 inhibitor 11j 对 hSMG-1 的选择性是 mTOR (IC50=50 nM)，PI3Kα/γ (IC50=92/60 nM) 和 CDK1/CDK2 (IC50=32/7.1 µM) 的 455 倍以上。hSMG-1 inhibitor 11j 可用于癌症研究。
  17. GC50719 FMF-04-159-R Potent inhibitor of CDK16 and CDK14 (IC50 values are 6 and 140 nM, respectively in kinase activity assay; IC50 = 563 nM for CDK14 in BRET assay)
  18. GC61008 LSN3106729 hydrochloride LSN3106729hydrochloride，Abemaciclib的代谢物，是一种具有抗肿瘤活性的CDK抑制剂。LSN3106729hydrochloride和CRBN配体可用于设计PROTACCDK4/6降解剂。
  19. GC60681 CDK7/9 tide CDK7/9tide是CDK7或CDK9的肽底物。
  20. GC60680 CDK5 inhibitor 20-223 CDK5inhibitor20-223是一种有效的CDK2和CDK5抑制剂，IC50分别为6.0和8.8nM。CDK5inhibitor20-223有潜力用于结肠直肠癌(CRC)的研究。
  21. GC60532 6-(Dimethylamino)purine

    6-二甲基氨基嘌呤,6-Dimethylaminopurine

     6-Dimethylaminopurine (N,N-Dimethyladenine) is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes.
  22. GC60324 Ribociclib D6

    LEE011-d6

     RibociclibD6(LEE011D6)是Ribociclib的一种氘代化合物。Ribociclib是一种高度特异性的CDK4/6抑制剂，IC50值分别为10nM和39nM，对cyclinB/CDK1复合体的活性低于其1000倍。
  23. GC39811 FIT-039 A Cdk9 inhibitor
  24. GC39421 PNU112455A hydrochloride A Cdk2 and Cdk5 inhibitor
  25. GC50615 BSJ-03-204 BSJ-03-204 是一种 PROTAC，由 Cereblon 和 CDK 的配体连接。 BSJ-03-204 是一种有效且选择性的基于 Palbociclib 的 CDK4/6 双降解剂 (PROTAC)，对 CDK4/D1 和 CDK6/D1 的 IC50 分别为 26.9 nM 和 10.4 nM。 BSJ-03-204 不诱导 IKZF1/3 降解并具有抗癌活性。
  26. GC50532 KuWal151 Potent and selective CLK inhibitor
  27. GC50484 TL 12-186 TL 12-186 是一种依赖于大脑的多激酶 PROTAC 降解剂。多激酶包括 CDK、BTK、FLT3、Aurora 激酶、TEC、ULK、ITK 等。 TL 12-186 抑制 CDK2/cyclin A (IC50\u003d73 nM) 和 CDK9/cyclin T1 (IC50\u003d55 nM)。
  28. GC50452 BRD 6989 A Cdk8/cyclin C complex inhibitor
  29. GC50239 ML 315 hydrochloride Inhibitor of Clk and DYRK kinases
  30. GC50217 BS 181 dihydrochloride BS 181 dihydrochloride 是一种比 Seliciclib 有效且选择性的 CDK7 抑制剂 (IC50\u003d21 nM)。 BS-181 还针对 CDK2、CDK5 和 CDK9，IC50 值分别为 880 nM、3000 nM 和 4200 nM（无法阻断 CDK1、4 和 6）。 BS 181 dihydrochloride 抑制一组癌细胞生长 (IC50\u003d11.5 μM-37.3 μM) 并诱导细胞凋亡。 BS 181 dihydrochloride 具有研究癌症治疗的潜力。
  31. GC39281 (R)-CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

     An inhibitor of cyclin-dependent kinases
  32. GC39175 SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors.
  33. GC39162 TCMDC-135051 TCMDC-135051 是一种高选择性和有效性的蛋白激酶 PfCLK3 抑制剂，具有低的靶外毒性。TCMDC-135051 可以防止滋养体到裂殖体的转变，破坏转录并减少向蚊子载体的传播。TCMDC-135051 具有抗寄生虫活性 (EC50=320 nM)。
  34. GC38899 CDK ligand for PROTAC hydrochloride CDK ligand for PROTAC hydrochloride 是一种具有抗肿瘤活性的 CDK 抑制剂。CDK ligand for PROTAC hydrochloride 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。
  35. GC45983 Voruciclib A pan-CDK inhibitor
  36. GC38755 CKI-7 A CK1 inhibitor
  37. GC38749 Abemaciclib metabolite M20

    LSN3106726

    Abemaciclib metabolite M20 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂，可用于癌症的相关研究
  38. GC38737 AS2863619 free base A dual inhibitor of Cdk8 and Cdk19
  39. GC38736 AS2863619 AS2863619是一种口服小分子环依赖性激酶（CDK）8和19抑制剂，IC50值分别为0.6099nM和4.277nM。
  40. GC38482 Desmethylglycitein

    4',6,7-三羟基异黄酮; 4',6,7-Trihydroxyisoflavone

     An active metabolite of daidzein
  41. GC38377 (2S,3R)-Voruciclib hydrochloride (2S,3R)-Voruciclib hydrochloride 是 Voruciclib hydrochloride 的低活性异构体。Voruciclib hydrochloride 是一种 CDK9 抑制剂。
  42. GC38330 EHT 5372 EHT 5372 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，其 IC50 值分别为 0.22，0.28 nM。
  43. GC37786 THZ1-R A non-cysteine reactive derivative of THZ1
  44. GC37709 SY-1365

    SY-1365

     SY-1365 (SY-1365) 是一种有效的一流的选择性 CDK7 抑制剂，Ki 为 17.4 nM。 SY-1365 在实体瘤细胞系中表现出抗增殖和凋亡作用。 SY-1365 在血液学和多种侵袭性实体瘤中具有抗肿瘤活性。
  45. GC37627 Senexin A Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.
  46. GC37529 Ribociclib succinate hydrate

    瑞柏司可里布(RIBOCICLIBLEE011)琥珀酸盐水合物,LEE011 succinate hydrate

     Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
  47. GC37523 RGB-286638 free base

    N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-C]吡唑-5-基]-N'-4-吗啉基脲

     A multi-kinase inhibitor
  48. GC37522 RGB-286638

    N-[1,4-二氢-3-[4-[[4-(2-甲氧基乙基)-1-哌嗪基]甲基]苯基]-4-氧代茚并[1,2-C]吡唑-5-基]-N'-4-吗啉基脲盐酸盐

     A multi-kinase inhibitor
  49. GC36892 PHA-767491 hydrochloride

    1,5,6,7-四氢-2-(4-吡啶基)-4H-吡咯并[3,2-C]吡啶-4-酮盐酸盐,CAY-10572 hydrochloride

     A potent Cdc7 kinase inhibitor
  50. GC36732 NG 52

    2-[[6-[(3-氯苯基)氨基]-9-异丙基-9H-嘌呤-2-基]氨基]乙醇,Compound 52

     An inhibitor of yeast cyclin-dependent kinases
  51. GC36313 Indirubin-5-sulfonate Indirubin-5-sulfonate 是周期蛋白依赖性激酶(CDK) 的抑制剂，对CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E、CDK4/cyclin D1 和CDK5/p35 的IC50 值分别为55 nM、35 nM、150 nM、300 nM 和 65 nM。Indirubin-5-sulfonate 同样能抑制GSK-3β 的活性。

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