Signaling Pathway

CDK

CDK

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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).

CDK Inhibitors & Modulators (68)

Product Name Catalog No. Brief Description
1-NM-PP1

HY-13942

1NM-PP1(PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors(IC50=28 uM vSrc; 4.2 nM v-Src-as1 I338G).

AMG 925

HY-15889

AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.

AT7519

HY-50940

AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AT7519 Hydrochloride

HY-50943

AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; is less potent to CDK3 and little active to CDK7.

AT7519 trifluoroacetate

HY-50940A

AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AZD-5438

HY-10012

AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM.

BIO

HY-10580

6-BIO(6-Bromoindirubin-3'-oxime) is a potent and selective inhibitor of GSK-3 and CDK1–cyclinB complex with IC50 of 5 nM /320 nM/83 nM for GSK-3αβ/CDK1/CDK5 respectively.

BMS-265246

HY-15275

BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.

Briciclib

HY-16366

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

BS-181

HY-13266

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM.

BS-181 hydrochloride

HY-13266A

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM.

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.

CDK-IN-2

HY-13033

CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM.

CDK9-IN-1

HY-13231

CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection.

CDK9-IN-2

HY-16462

CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor.

CDK9-IN-6

HY-12214

CDK9-IN-6 is a CDK9 inhibitor, refers to Example 399 in WO 2012101062 A1

CDKI-73

HY-12445

CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).

CVT-313

HY-15339

CVT-313(NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 (IC50 = 0.5 uM for Cdk2/A and Cdk2/E; 4.2 uM for Cdk1/B; 215 uM for Cdk4/D1).

Dinaciclib

HY-10492

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.

Flavopiridol

HY-10005

Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM.