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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
CDK2-IN-22 V84559 CDK2-IN-22
CDK2-IN-24 V83483 CDK2-IN-24
CDK2-IN-3 V55071 CDK2-IN-3 222035-13-4 CDK2-IN-3 (compound 3) is a potent and specific CDK2 inhibitor at 50 and 60 nM.
CDK2-IN-7 V55097 CDK2-IN-7 2498658-13-0 CDK2-IN-7 is a CDK2 inhibitor (IC50 < 50 nM) for cancer research.
CDK2-IN-8 V75988 CDK2-IN-8 2919216-36-5 CDK2-IN-8 is a potent CDK2 inhibitor (antagonist) with IC50 of 1.74 µM.
CDK2-IN-9 V75989 CDK2-IN-9 2919216-33-2 CDK2-IN-9 is a potent CDK2 inhibitor (antagonist) with IC50 of 0.63 µM.
CDK2/4/6-IN-1 V52283 CDK2/4/6-IN-1 2803837-13-8 CDK2/4/6-IN-1 (example 29) is a CDK2/4/6 inhibitor (antagonist) with IC50s of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6 respectively, may be utilized in cancer research.
CDK2/4/6-IN-2 V55105 CDK2/4/6-IN-2 2531748-80-6 CDK2/4/6-IN-2 is a CKD2/4/6 inhibitor (antagonist) with IC50s: less than 1 μM, less than 10 nM, and less than 100 nM.
CDK2/Bcl2-IN-1 V77912 CDK2/Bcl2-IN-1 CDK2/Bcl2-IN-1 (compound 1) is a saponin and a CDK-2 inhibitor (IC50=117.6 nM) with good cytotoxic effect against cancer cells.
Cdk2/Cyclin Inhibitory Peptide I V52282 Cdk2/Cyclin Inhibitory Peptide I 237392-84-6 Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) is a CDK2 inhibitor that kills U2OS osteosarcoma cells in a dose-dependent fashion.
Cdk2/Cyclin Inhibitory Peptide II V52281 Cdk2/Cyclin Inhibitory Peptide II 237392-85-7 Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL) is a CDK2 inhibitor that kills U2OS osteosarcoma cells in a dose-dependent fashion.
CDK4-IN-2 V55080 CDK4-IN-2 2380320-68-1 CDK4-IN-2 (A17) is an inhibitor (blocker/antagonist) of CDK4 with both Ki and IC50s less than 10 nM.
CDK4/6-IN-13 V75979 CDK4/6-IN-13 1908454-70-5 As a CDK4/6 inhibitor.
CDK4/6-IN-14 V52280 CDK4/6-IN-14 2699091-15-9 CDK4/6-IN-14 is a potent and selective inhibitor of CDK4 and CDK6 (CDK) with IC50 of 10 nM and 16 nM, respectively.
CDK4/6-IN-15 V52279 CDK4/6-IN-15 2078047-99-9 CDK4/6-IN-15 is an orally bioactive and selective CDK4/6 inhibitor.
CDK4/6-IN-16 V55088 CDK4/6-IN-16 1169694-98-7 CDK4/6-IN-16 (example 195) is a potent inhibitor of CDK4 and CDK6 with IC50 of 0.013 μM for CDK4.
CDK4/6-IN-17 V55095 CDK4/6-IN-17 2035069-96-4 CDK4/6-IN-17 (compound 12) is an orally bioactive CDK4/6 inhibitor (antagonist) with IC50 range 10-100 nM in BE(2) cells.
CDK4/6-IN-3 V52278 CDK4/6-IN-3 2366237-37-6 CDK4/6-IN-3 is a brain-penetrating CDK4/CDK6 inhibitor (antagonist) with Ki of <0.3 nM and 2.2 nM respectively.
CDK4/6-IN-4 V41999 CDK4/6-IN-4 2138499-06-4 Abemaciclib metabolite M20 (LSN3106726) is the bioactive metabolite of Abemaciclib and a selective CDK4/6 inhibitor that may be utilized in cancer-related research.
CDK4/6-IN-5 V52277 CDK4/6-IN-5 2380321-50-4 CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor (antagonist) with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3.
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