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

Cat.No. 产品名称 Information
GC38755 CKI-7 A CK1 inhibitor
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
GC38737 AS2863619 free base A dual inhibitor of Cdk8 and Cdk19
GC38736 AS2863619 A dual inhibitor of Cdk8 and Cdk19
GC38482 Desmethylglycitein
4',6,7-三羟基异黄酮; 4',6,7-Trihydroxyisoflavone
An active metabolite of daidzein
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。
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。
GC37786 THZ1-R A non-cysteine reactive derivative of THZ1
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。
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.
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.
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
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
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
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
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。
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。
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。
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。
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。
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。
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。
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。
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.
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。
GC35512 BI-1347 BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM.
GC35315 AMG 925 HCl A dual inhibitor of FLT3 and Cdk4
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。
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。
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。
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。
GC43175 CAY10574 A Cdk2-cyclin E and Cdk9 inhibitor
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
GC34692 NU6140 A Cdk2 inhibitor
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.
GC40092 PD 0332991-d8
帕博西尼-D8,PD 0332991-d8
An internal standard for the quantification of PD 0332991
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。
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。
GC34355 SEL120-34A monohydrochloride A dual inhibitor of Cdk8 and Cdk19
GC34204 JSH-150 JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
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.
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.
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.
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。
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。
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.
GC34056 NVP-2 A Cdk9/cyclin T1 complex inhibitor
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。
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。
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。