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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
CDK8-IN-17 V104741 CDK8-IN-17 451458-32-5 CDK8-IN-17 (Compound WS-2) is a CDK8 inhibitor with IC50 of 9 nM, which can be used in cancer research.
CDK8-IN-5 V75992 CDK8-IN-5 2855087-10-2 CDK8-IN-5 is a potent inhibitor of CDK8 with IC50 of 72 nM.
CDK8-IN-9 V75978 CDK8-IN-9 2850253-95-9 CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor (antagonist) with IC50 of 48.6 nM.
CDK9 inhibitor HH1 V55103 CDK9 inhibitor HH1 204188-41-0 CDK9 inhibitor HH1 is a potent and specific CDK9 inhibitor.
CDK9-Cyclin T1 PPI-IN-1 V79317 CDK9-Cyclin T1 PPI-IN-1 CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor.
CDK9-IN-11 V75993 CDK9-IN-11 2748368-15-0 CDK9-IN-11 is a potent CDK9 inhibitor.
CDK9-IN-12 V55096 CDK9-IN-12 1942843-54-0 CDK9-IN-12 showed the best CDK9 inhibitory activity with IC50 of 5.41 nM.
CDK9-IN-13 V75984 CDK9-IN-13 2768712-71-4 CDK9-IN-13 (compound 38) is a potent and specific CDK inhibitor (antagonist) with IC50 <3 nM.
CDK9-IN-22 V52268 CDK9-IN-22 2872677-61-5 CDK9-IN-22 is a potent CDK9 inhibitor (antagonist) with IC50s of 10.4 and 876.2 nM for CDK9 and CDK, respectively.
CDK9-IN-23 V55087 CDK9-IN-23 2761572-96-5 CDK9-IN-23 (Example 4) is a CDK9 inhibitor (antagonist) with IC50 <20 nM.
CDK9-IN-24 V78623 CDK9-IN-24 CDK9-IN-24 (compound 21a) is a selective CDK9 inhibitor (antagonist) with significant inhibitory effect on tumor growth.
CDK9-IN-26 V80215 CDK9-IN-26 CDK9-IN-26 (compound 1d) is a CDK9 inhibitor (IC50=0.18 μM).
CDK9-IN-27 V78705 CDK9-IN-27 CDK9-IN-27 (Compound 6a) is a CDK9 inhibitor (IC50s: 0.424 μM).
CDK9-IN-28 V78706 CDK9-IN-28 CDK9-IN-28 (compound 10) is a potent CDK9 inhibitor.
CDK9-IN-29 V75977 CDK9-IN-29 2737262-24-5 CDK9-IN-29 is a potent CDK9 inhibitor (IC50 = 3.20 nM) with good kinase selectivity.
CDK9-IN-30 V75983 CDK9-IN-30 748146-89-6 CDK9-IN-30 is a CDK9 inhibitor that can suppress the replication of HIV-1 virus.
CDK9-IN-31 V85741 CDK9-IN-31 2991074-93-0
CDK9-IN-31 dimaleate V85719 CDK9-IN-31 dimaleate
CDK9-IN-35 V94540 CDK9-IN-35 CDK9-IN-35 (Compound 10j) is an inhibitor of CDK9/Cyclin T1 with IC50 of 10.2 nM and IC50 of 20 nM for HCT-116 cell line.
CDK9-PROTAC V3574 CDK9-PROTAC 2118356-96-8 CDK9-PROTAC (PROTAC CDK9 Degrader-1) is a novel, potent and selective CDK9(Cyclin-dependent kinase 9) degrader.
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