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
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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。
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
GC14974
AMG 925
A dual inhibitor of FLT3 and Cdk4
-
GC12011
P276-00
P276-00
P276-00 (P276-00) 是一种有效的细胞周期蛋白依赖性激酶 (CDK) 抑制剂,可抑制 CDK9-cyclinT1、CDK4-cyclin D1 和 CDK1-cyclinB,IC50 分别为 20 nM、63 nM 和 79 nM。 P276-00 (P276-00) 对顺铂耐药细胞具有抗肿瘤活性。 -
GC17400
R547
[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮
A selective Cdk inhibitor -
GC10842
LEE011
瑞博西尼; LEE011
A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor -
GC16425
Flavopiridol hydrochloride
(-)-2-(2-氯苯基)-5,7-二羟基-8-[(3S,4R)-3-羟基-1-甲基-4-哌啶基]-4H-1-苯并吡喃-4-酮盐酸盐,Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride
An inhibitor of cyclin-dependent kinases -
GC16268
Purvalanol B
(2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇,NG 95; NG95; NG-95
A CDK inhibitor -
GC17648
Dinaciclib(SCH727965)
(2S)-1-[3-乙基-7-[[(1-氧代-3-吡啶基)甲基]氨基]吡唑并[1,5-A]嘧啶-5-基]-2-哌啶乙醇,SCH 727965
A CDK inhibitor -
GC12865
BMS265246
A cell-permeable inhibitor of Cdk1 and Cdk2
-
GC15588
PHA-848125
PHA-848125
An inhibitor of Cdks -
GC15421
Palbociclib (PD0332991) Isethionate
帕博西尼羟乙基磺酸盐; PD 0332991 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。 -
GC12438
AZD-5438
4-[2-甲基-1-异丙基-1H-咪唑-5-基]-N-[4-(甲磺酰基)苯基]-2-嘧啶胺,AZD 5438;AZD5438
A potent inhibitor of CDKs -
GC17935
PD 0332991 (Palbociclib) HCl
帕布昔利布盐酸盐,PD0332991;PD-0332991;PD 0332991
PD 0332991 作为 CDK4 和 CDK6 激酶的口服活性强效和高选择性抑制剂,可以在低纳摩尔浓度下阻断 pRb 磷酸化并随后在敏感细胞系中诱导 G1 期停滞。 -
GC16822
LY2835219
Abemaciclib; LY2835219 methanesulfonate
LY2835219 free base是 CDK4 和 CDK6 的强效选择性抑制剂,在非细胞实验中的 IC50 分别为 2nM 和 10nM。 -
GC15870
AT7519
4-[(2,6-二氯苄基)氨基]-N-4-哌啶1H-吡唑-3-羧胺,AT7519M
A Cdk inhibitor -
GC13690
BS-181 HCl
A selective Cdk7 inhibitor
-
GC15047
PHA-793887
3-甲基-N-[1,4,5,6-四氢-6,6-二甲基-5-[(1-甲基-4-哌啶基)甲酰基]吡咯并[3,4-C]吡唑-3-基]丁酰胺
A CDK inhibitor