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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
BSJ-03-204 V52316 BSJ-03-204 2349356-09-6 BSJ-03-204 is a PROTAC linked by Cereblon ligand and CDK ligand.
BSJ-04-132 V52315 BSJ-04-132 2349356-39-2 BSJ-04-132 is a PROTAC linked by Cereblon ligand and CDK ligand.
BSJ-5-63 V92099 BSJ-5-63 2519823-37-9 BSJ-5-63 is a potent CDK12, CDK7, and CDK9 degrader.
CAF-382 V80116 CAF-382 CAF-382 (compound B1) is an SNS-032 analogue and a CDKL5 and pan-CDK inhibitor (antagonist) with weak GSK3α/β affinity (>1.8 μM) and inhibitory activity.
CAY-10572 V0062 PHA 767491 845714-00-3 PHA-767491 (formerly also called CAY10572) is a novel and potent ATP-competitive dual inhibitor of Cdc7/CDK9 with IC50 of 10 nM and 34 nM in cell-free assays, respectively.
CC-671 V17707 CC-671 1618658-88-0 CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor (antagonist) with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.
Cdc7-IN-20 V89476 Cdc7-IN-20 Cdc7-IN-20 (EP-05) is an orally available, selective Cdc7 inhibitor with IC50 and Ki values of 0.93 and 0.11 nM, respectively.
Cdc7-IN-3 V55075 Cdc7-IN-3 1402057-87-7 Cdc7-IN-3 (compound IA) is a potent Cdc7 kinase inhibitor.
Cdc7-IN-4 V55072 Cdc7-IN-4 1402059-21-5 Cdc7-IN-4 (compound IC) is a potent Cdc7 kinase inhibitor.
Cdc7-IN-5 V53128 Cdc7-IN-5 1402057-86-6 Cdc7-IN-5 (compound IB) is a potent Cdc7 kinase inhibitor.
Cdc7-IN-7 V55074 Cdc7-IN-7 1402059-17-9 Cdc7-IN-7 (compound IE) is a potent Cdc7 kinase inhibitor.
CDD-2807 V88786 CDD-2807 CDD-2807 is a serine/threonine kinase 33 (STK33) inhibitor with an IC50 of 9.2 nM.
CDDD11-8 V85750 CDDD11-8 2241659-94-7
CDK-IN-11 V84992 CDK-IN-11 2376876-87-6
CDK-IN-12 V55084 CDK-IN-12 2789680-97-1 CDK-IN-12 (Example 20) is a CDK inhibitor.
CDK-IN-13 V85556 CDK-IN-13
CDK-IN-15 V94528 CDK-IN-15 3036232-03-5 CDK-IN-15 (Compound 456) is a potent Cyclin A inhibitor with IC50 value of 0.14 μM.
CDK-IN-16 V105098 CDK-IN-16 CDK-IN-16 (Compound 5g) is a CDK2/Cyclin A2 inhibitor with IC50 of 1.67 μM.
CDK-IN-6 V35035 CDK-IN-6 779353-02-5 CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compounds, is a CDK inhibitor (antagonist) with anti-cancer effect.
CDK/HDAC-IN-1 V55100 CDK/HDAC-IN-1 2762181-73-5 CDK/HDAC-IN-1 showed significant inhibitory effect against CDK2/4/6 and HDAC6 (IC50 = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM).
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