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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
CDK4 degrader 1 V102237 CDK4 degrader 1 CDK4 Degrader 1 (ML 1–71) is a monovalent degrader targeting CDK4.
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-15 hydrochloride V89568 CDK4/6-IN-15 hydrochloride CDK4/6-IN-15 hydrochloride is an orally available selective inhibitor of CDK4/6.
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-18 V102563 CDK4/6-IN-18 546102-60-7 CDK4/6-IN-18 (Example 2BrIC) is a selective CDK4/6 inhibitor.
CDK4/6-IN-19 V88614 CDK4/6-IN-19 3033950-86-3 CDK4/6-IN-19 (Compound II-7) is a CDK4/CDK6 inhibitor with IC50 values of 0.2, 5.0 nM, respectively.
CDK4/6-IN-20 V92049 CDK4/6-IN-20 3033950-84-1 CDK4/6-IN-20 (Compound II-5) is a CDK4/CDK6 inhibitor with IC50 values of 1.9, 14.2 nM, respectively.
CDK4/6-IN-21 V99718 CDK4/6-IN-21 2102887-41-0 CDK4/6-IN-21 (Compound I-52) is a CDK4/6 inhibitor with IC50 values of 3.88 and 3.31 nM for CDK4 and CDK6, respectively.
CDK4/6-IN-21 maleate V92033 CDK4/6-IN-21 maleate 2765997-88-2 CDK4/6-IN-21 maleate (compound I-52) is a CDK4/6 inhibitor with IC50 values of 3.88 and 3.31 nM for CDK4 and CDK6, respectively.
CDK4/6-IN-22 V99607 CDK4/6-IN-22 3036014-62-4 CDK4/6-IN-22 (Compound 1-A) is a dual inhibitor of CDK4 and CDK6.
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.
CDK5-IN-1 V55093 CDK5-IN-1 2639540-19-3 CDK5-IN-1 is a potent CDK5 inhibitor (antagonist) with less than 10 nM activity against CDK5.
Cdk5i peptide V88611 Cdk5i peptide 2298317-00-5 Cdk5i peptide is a 12 amino acid long peptide fragment from Cdk5.
CDK7-IN-1 V96978 CDK7-IN-1 1957203-02-9 CDK7-IN-1 is an analog of YKL-5-124, a cyclin-dependent kinase 7 (cdk7) inhibitor with an IC50 value of less than 100 nM, from patent WO 2016105528 A2 compound example 215.
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