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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
CDK7-IN-10 V55101 CDK7-IN-10 2588110-62-5 CDK7-IN-10 is a CDK7 inhibitor (antagonist) with IC50 of less than 100 nM, found in patent WO2021016388A1, compound I-1.
CDK7-IN-11 V52275 CDK7-IN-11 2414896-32-3 CDK7-IN-11 is an orally bioactive CDK7 inhibitor.
CDK7-IN-2 hydrochloride hydrate V55073 CDK7-IN-2 hydrochloride hydrate 2326428-24-2 CDK7-IN-2 HCl hydrate (Example 6) is a potent and specific CDK7 inhibitor.
CDK7-IN-21 V55092 CDK7-IN-21 2766124-39-2 CDK7-IN-21 (compound A22) is a potent CDK7 inhibitor.
CDK7-IN-22 V55094 CDK7-IN-22 2173190-60-6 CDK7-IN-22 (compound 101) is a CDK7 inhibitor (antagonist) with anti-tumor activity.
CDK7-IN-25 V55089 CDK7-IN-25 2009209-60-1 CDK7-IN-25 (CY-16-1) is a CDK-7 inhibitor (IC50<1nM) and may be utilized in cancer-related research.
CDK7-IN-26 V78702 CDK7-IN-26 CDK7-IN-26 (compound 36) is an orally bioactive CDK7 inhibitor (IC50= 7.4 nM).
CDK7-IN-27 V88613 CDK7-IN-27 CDK7-IN-27 (Compound 37) is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) with a Ki of 3 nM.
CDK7-IN-28 V89495 CDK7-IN-28 CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor (IC50<5 nM).
CDK7-IN-29 V101017 CDK7-IN-29 3024545-83-0 CDK7-IN-29 (Compound 20) is an inhibitor of CDK7 with IC50 of 1.4 nM.
CDK7-IN-32 V105045 CDK7-IN-32 2055741-42-7 CDK7-IN-32 (Compound 10) is an inhibitor of CDK7.
CDK7-IN-5 V52274 CDK7-IN-5 1817006-50-0 CDK7-IN-5 is a CDK7 inhibitor (antagonist) with IC50 <100 nM.
CDK7-IN-6 V52273 CDK7-IN-6 2378710-04-2 CDK7-IN-6 is a potent and specific cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), found in patent WO2019197549 A1, compound 210.
CDK7-IN-7 V52272 CDK7-IN-7 2640208-01-9 CDK7-IN-7 is a potent CDK7 inhibitor (antagonist) with IC50 of <50 nM.
CDK7/9 tide V77159 CDK7/9 tide CDK7/9 tide is a bioactive peptide substrate of CDK7 or CDK9.
CDK7/9-IN-1 V52276 CDK7/9-IN-1 2747919-19-1 CDK7/9-IN-1 is a cyclin-dependent kinase 7/9 (CDK7/9) inhibitor.
CDK8-IN-11 V52271 CDK8-IN-11 2839338-28-0 CDK8-IN-11 is a potent and specific inhibitor of CDK8 with IC50 of 46 nM.
CDK8-IN-12 V52270 CDK8-IN-12 2613307-67-6 CDK8-IN-12 is an orally bioactive and potent CDK8 inhibitor (antagonist) with Ki of 14 nM.
CDK8-IN-15 V101635 CDK8-IN-15 2988020-03-5 CDK8-IN-15 (compound 46) is a potent CDK8 inhibitor with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8, inhibit NF-κB, and selectively inhibit the CDK family and tyrosine. In addition, it can also play a positive role in TNF-α-induced psoriasis in vitro, enhance the expression of Foxp3 and IL-10, and reduce inflammatory response. It is expected to be applied to the study of psoriasis.
CDK8-IN-16 V105329 CDK8-IN-16 1860885-61-5 CDK8-IN-16 (Compound 51) is an orally active dual inhibitor of CDK8 and CDK19 with IC50 of 5.1 nM and 5.6 nM, respectively.
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