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
- 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。
- 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。
- GC33137 SEL120-34A A dual inhibitor of Cdk8 and Cdk19
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GC33107
(±)-BAY-1251152
(±)-BAY-1251152; (±)-VIP152
A racemic mixture of (+)-BAY-1251152 and (–)-BAY-1251152 - 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.
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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。
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GC32930
Simurosertib (TAK-931)
TAK-931
An inhibitor of Cdc7 kinase - GC32898 SEL120-34A HCl A dual inhibitor of Cdk8 and Cdk19
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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。 -
GC32832
PF-06873600
PF-3600
An inhibitor of Cdk2, Cdk4, and Cdk6 - GC32829 NU6300 NU6300是一种共价的ATP竞争性CDK2抑制剂。
- GC32746 MSC2530818 A Cdk8 inhibitor
- 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。
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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. - 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.
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GC32700
CYC065
CYC065
An inhibitor of Cdk2 and Cdk9 -
GC32429
(-)-BAY-1251152
(-)-BAY-1251152; (-)-VIP152
A racemic mixture of (+)-BAY-1251152 and (–)-BAY-1251152 - GC30977 Ca2+ channel agonist 1 Ca2+channelagonist1是一种N-型钙离子通道(N-typeCa2+channel)激动剂和Cdk2的抑制剂,EC50分别为14.23μM和3.34μM,对运动神经终端功能障碍有潜在疗效。
- GC30466 CDK8-IN-3 CDK8-IN-3是CDK8的抑制剂,来自专利WO2016041618A1,化合物实例1.7。
- GC30245 CLK1-IN-1 CLK1-IN-1是一个有效的、Cdc2-like激酶(CLK1)的选择性抑制剂,其IC50值为2nM。
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GC19326
Senexin B
4-[[2-[6-[(4-甲基-1-哌嗪基)羰基]-2-萘基]乙基]氨基]-6-喹唑啉甲腈
An inhibitor of Cdk8 and Cdk19 -
GC19267
NU2058
O6-(Cyclohexylmethyl)guanine
An inhibitor of Cdk1 and Cdk2 - GC19233 LY3177833 An inhibitor of Cdc7 kinase
- GC19219 LDC4297 A CDK7 inhibitor
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GC19096
CDKI-73
LS-007
CDKI-73 (LS-007) 是一种具有口服活性且高效的 CDK9 抑制剂,对 CDK9、CDK1 和 CDK2 的 Ki 值分别为 4 nM、4 nM 和 3 nM。 - GC19089 CC-671 A dual inhibitor of Mps1/TTK and Clk2
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GC19067
BGG463
K03859
BGG463 (K03859) 是一种具有口服活性的 II 型 CDK2 抑制剂。 -
GC18354
Bisindolylmaleimide X (hydrochloride)
BIM-X hydrochloride; Ro31-8425 hydrochloride
A PKC inhibitor -
GC15841
Alsterpaullone
阿特波龙,9-Nitropaullone,NSC 705701
A dual CDK and GSK3 inhibitor - GC11022 SB 218078 A potent Chk1 inhibitor
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GC15607
ON123300
8-环戊基-7,8-二氢-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-7-氧代-吡啶并[2,3-D]嘧啶-6-甲腈,ON123300
A multi-kinase inhibitor - GC16420 THZ531 An inhibitor of Cdk12 and Cdk13
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GC14230
K03861
AUZ454或者K03861,K03861
K03861 (K03861) 是一种 II 型 CDK2 抑制剂,Kd 为 8.2 nM。 K03861 (K03861) 通过与活化细胞周期蛋白的结合竞争抑制 CDK2 活性。 - GC13511 THZ2 A Cdk7 inhibitor
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GC14707
Purvalanol A
NG-60
A selective inhibitor of cyclin-dependent kinases -
GC12348
Ro 3306
2-[[(噻吩-2-基)甲基]氨基]-5-[1-(喹啉-6-基)甲-(Z)-亚基]噻唑-4-酮
An inhibitor of Cdk1 - GC16511 OTS964 A TOPK inhibitor
- GC11971 LY2857785 A Cdk9 inhibitor
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GC17067
LDC000067
(3-(6-(2-甲氧基苯基)嘧啶-4-基氨基)苯基)甲烷磺酰胺,LDC067
A Cdk9 inhibitor - GC11774 KH CB19 KH CB19 是一种有效的 CLK(cdc2 样激酶)抑制剂(CLK1 IC50\u003d19.7 nM;CLK3 IC50\u003d530 nM)。
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GC11040
Borrelidin
疏螺旋体素,Treponemycin
An antiangiogenic antibiotic -
GC14182
Kenpaullone
克莱拉尼,9-Bromopaullone; NSC-664704
A inhibitor of cyclin-dependent kinase and GSK3β - GC12642 THZ1 Hydrochloride A covalent Cdk7 inhibitor
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GC14162
ML167
5-[4-[[(5-甲基-2-呋喃基)甲基]氨基]-6-喹唑啉基]-2-呋喃甲醇,CID44968231; NCGC00188654
A selective Clk4 inhibitor - GC10840 THZ1 A covalent Cdk7 inhibitor
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GC14987
GSK-3 Inhibitor IX (BIO)
(2'Z,3'E)-6-溴靛玉红-3'-肟,GSK-3 Inhibitor IX
A potent, selective, and reversible GSK3 inhibitor -
GC15377
LEE011 succinate
瑞博西尼琥珀酸盐; LEE011 succinate
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor -
GC15922
LEE011 hydrochloride
瑞博西尼盐酸盐; LEE011 hydrochloride
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor -
GC13328
XL413 hydrochloride
BMS-863233 hydrochloride
A potent inhibitor of Cdc7 - GC18117 XL413 A potent inhibitor of Cdc7