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CDK

CDKs (Cyclin-dependent kinases) are a family of protein kinases first discovered for their role in regulating the cell cycle. Types: Cdk1, Cdk2, Cdk3, Cdk4, Cdk5, Cdk6, Cdk7, Cdk8, Cdk9, Cdk11. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are present in all knowneukaryotes, and their regulatory function in the cell cycle has been evolutionarily conserved. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. 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. CDKs phosphorylate their substrates on serines and threonines, so they are serine-threonine kinases. CDK levels remains 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. cerevisiae (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).

Cyclin-dependent kinase (71)
产品名称 目录号 简述
1-NM-PP1 HY-13942

1NM-PP1(PP1 Analog II)是可渗透入细胞的PP1类似物,可选择性抑制突变型激酶,对v-Src-as1 I338G和vSrc的IC50分别为4.2 nM和28 uM。

AMG 925 HY-15889

AMG 925是CDK4/FLT3双重抑制剂,IC50分别为1.5 nM和2.4 nM,对MOLM-13细胞的IC50为19 nM。

AT7519 HY-50940

AT7519是CDK抑制剂,对CDK1,2,4,6和9的IC50为10-210 nM,对CDK3的抑制性较低,而对CDK7则几乎无抑制性。

AT7519 Hydrochloride HY-50943

AT7519盐酸盐是CDK抑制剂,对CDK1,2,4,6和9的IC50为10-210 nM,对CDK3的抑制性较低,而对CDK7则几乎无抑制性。

AT7519 trifluoroacetate HY-50940A

AT7519三氟醋酸盐是CDK抑制剂,对CDK1,2,4,6和9的IC50为10-210 nM,对CDK3的抑制性较低,而对CDK7则几乎无抑制性。

AZD-5438 HY-10012

AZD5438是CDK1,2,9的抑制剂,IC50分别为16 nM,6 nM,20 nM,对CDK5和6的抑制性较弱。

BAY-1143572 HY-12871

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

BIO HY-10580

6-BIO(6-Bromoindirubin-3_acute_-oxime)是一个有效、选择性GSK-3_alpha_/_beta_)、CDK1-cyclinB和CDK5抑制剂,IC50值分别为5nM、320nM和83nM。

BMS-265246 HY-15275

BMS-265246是CDK1/2抑制剂,对CDK1/cyclin B和CDK2/cyclin E的IC50分别为6 nM和9 nM。

Briciclib HY-16366

Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.

BS-181 HY-13266

BS-181是高选择性CDK7抑制剂,IC50为21 nM,比对CDK1,2,4,5,6和9的抑制性强超过40倍。

BS-181 hydrochloride HY-13266A

BS-181盐酸盐是CDK7高效选择性抑制剂,IC50值21nM,对CDK1/92/4/5/6/9作用弱。

Ca2+ channel agonist 1 HY-41076

Ca2+ channel agonist 1 is a N-type Ca2+ channel activity agonist, with EC50 of 14.23 uM, also inhibits cdk2 kinase activity with EC50 of 3.34 uM.

CCT-251921 HY-19984

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.

CDK-IN-2 HY-13033

CDK-IN-2是CDK特异性抑制剂。

CDK9-IN-1 HY-13231

CDK9-IN-1是新型CDK9抑制剂,有抗HIV活性。

CDK9-IN-2 HY-16462

CDK9-IN-2是CDK9抑制剂。

CDK9-IN-6 HY-12214

CDKI-73 HY-12445

CDKI-73是CDK9高效抑制剂,Ki值为4nM,对CLL细胞株有选择性毒性作用,LD50值为80nM,对正常B细胞作用基本无。

CVT-313 HY-15339

CVT-313(NG-26)是可逆的ATP竞争性CDK2抑制剂,对Cdk2/A,Cdk1/B和Cdk4/D1的IC50分别为0.5 uM,4.2 uM和215 uM。

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