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CDK

CDK

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle.Additionally, they control mRNA processing, transcription, and nerve cell differentiation. With molecular weights between 34 and 40 kDa, CDKs are relatively small proteins that only contain the kinase domain. In fact, when their CDK gene has been replaced with the homologous human gene, yeast cells can proliferate normally. A CDK by definition binds the control protein cyclin. Only the cyclin-CDK complex is an active kinase; CDK lacks much kinase activity on its own.

Around 20 Cyclin-dependent kinases (CDK1-20) have been identified as of yet. While CDK 7, 8, 9 and 11 are linked to transcription, CDK1, 4, and 5 are involved in the cell cycle.

The majority of CDK regulation occurs post-translationally, and CDK levels are essentially constant throughout the cell cycle. The majority of knowledge about CDK structure and function is based on CDKs from vertebrates (CDC2 and CDK2), S. pombe (CDC28), and S. cerevisiae (Cdc2). Cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and CDK inhibitory subunit (CKI) binding are the four main mechanisms of CDK regulation.

CDK related products

Structure Cat No. Product Name CAS No. Product Description
hSMG-1 inhibitor 11j V24310 hSMG-1 inhibitor 11j 1402452-15-6 hSMG-1 inhibitor 11j, a pyrimidine analogue, is a potent and specific hSMG-1 inhibitor (antagonist) with IC50 of 0.11 nM.
Indirubin-3-oxime (IDR-3O) V51040 Indirubin-3-oxime (IDR-3O) 667463-82-3 Indirubin-3′-oxime (IDR3O), a synthetic indirubin derivative, is a novel inhibitor of glycogen synthase kinase 3β (GSK3β) and cyclin-dependent kinases (CDKs).
Inixaciclib V55077 Inixaciclib 2370913-42-9 Inixaciclib is a potent CDK inhibitor that may be utilized in anti-cancer research.
INX-315 V85794 INX-315 2745060-92-6
Ipivivint V51944 Ipivivint 1481617-15-5 Ipivivint (compound 38) is a potent CDC-like kinase (CLK) inhibitor (antagonist) with EC50s of 1 nM and 7 nM for CLK2 and CLK3, respectively.
IV-361 V51930 IV-361 2055741-39-2 IV-361 is an orally bioactive, selective CDK7 inhibitor (Ki≤50 nM).
JA397 V85475 JA397
JH-XVI-178 V53248 JH-XVI-178 2648453-53-4 JH-XVI-178 is a potent and specific CDK8/19 inhibitor (antagonist) with low clearance and moderate oral pharmacokinetic properties.
JSH-009 V92030 JSH-009 2247481-08-7 JSH-009 is a novel, highly selective inhibitor of CDK9, which is critical for regulating transcription elongation.
JSH-009 dimaleate V92031 JSH-009 dimaleate 2559759-04-3 JSH-009 dimaleate (Compound 1) is a potent and highly selective CDK9 inhibitor with IC50 of 0.928 nM.
JSH-150 V22999 JSH-150 2247481-21-4 JSH-150 is a potent and specific CDK9 inhibitor (antagonist) with IC50 of 1 nM.
K00546 V51912 K00546 443798-47-8 K00546 is a potent CDK1 and CDK2 inhibitor (antagonist) with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively.
K03861 (AUZ 454) V1536 K03861 (AUZ 454) 853299-07-7 K03861 (K0 3861;AUZ-454;K-03861;AUZ 454), an aminopyrimidine-phenyl urea analog, is novel and potent type IIcyclin-dependent kinase-CDK2 inhibitor with potential anticancer activity.
KB-0742 dihydrochloride V51906 KB-0742 dihydrochloride 2416874-75-2 KB-0742 di-HCl is a specific and orally bioactive CDK9 inhibitor (antagonist) with IC50 of 6 nM against CDK9/cyclin T1.
KH-CB20 V51903 KH-CB20 1354448-60-4 KH-CB20, an E/Z mixture, is a potent and specific inhibitor of CLK1 and the closely related isoform CLK4, with IC50 for CLK1 inhibition of 16.5 nM.
KuWal151 V84703 KuWal151 2341841-06-1
LDC000067 (LDC067) V1544 LDC000067 (LDC067) 1073485-20-7 LDC000067 (also called LDC-000067;LDC-067) is a novel, potent, highly selective and ATP-competitive inhibitor ofcyclin-dependent kinase (CDK9)with potential antineoplastic activity.
LDC4297 V2731 LDC4297 1453834-21-3 LDC4297 is a novel and potentCDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13±0.06 nM for CDK7and IC50s between 10 nM and 10,000 nM for all other analyzed CDKs.
LDC4297 hydrochloride V51877 LDC4297 hydrochloride 2319747-14-1 LDC4297 HCl is a selective inhibitor of CDK7 with IC50 of 0.13 nM.
LEE011 Succinate V3925 RIBOCICLIB SUCCINATE (LEE011) 1374639-75-4 Ribociclib succinate (LEE011; NVP-LEE-011; LEE-011, NVP-LEE011; Kisqali), the succinate salt of Ribociclib, is a CDK4/6 (cyclin-dependent kinase) inhibitor (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA for the treatment of breast cancer.
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