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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
RSS0680 V53079 RSS0680 2769753-48-0 RSS0680 (Example 22) is a bifunctional compound targeting protein-degrading kinases.
Samuraciclib HCl (ICEC0942; PPDA-001; CT7001) V5212 Samuraciclib HCl (ICEC0942; PPDA-001; CT7001) 1805789-54-1 Samuraciclib HCl (ICEC-0942; PPDA001; CT-7001), the hydrochloride salt of Samuraciclib, is a novel, potent, orally bioavailable and selective CDK7 inhibitor with potential anticancer activity.
SB-1295 V79248 SB-1295 SB-1295 is an orally bioactive CDK9/T1 inhibitor (IC50=0.17 μM).
SEL120-34A HCl V4557 SEL120-34A HCl 1609452-30-3 SEL120-34A hydrochloride (SEL-120-34A; SEL12034A) is a novel, potent and selective ATP-competitiveinhibitor of CDK8(Cyclin-dependent kinase 8) with anticancer activity.
SEL120-34A monohydrochloride V37095 SEL120-34A monohydrochloride 2443816-41-7 SEL120-34A mono HCl is a selective, ATP-competitive CDK8 inhibitor (antagonist) with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC complexes, respectively, and a Kd of 3 nM for CDK8.
Seliciclib (Roscovitine) V1532 Seliciclib (Roscovitine) 186692-46-6 Seliciclib (also known as Roscovitine, CYC 202; CYC-202;CYC202) is a novel, potent, selective and orally bioavailable small-molecule CDK inhibitor with potential anticancer activity.
Senexin A V2743 Senexin A 1366002-50-7 Senexin A is a novel, potent, selective and ATP site competitive inhibitor of CDK8 and CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19, respectively.
Senexin A hydrochloride V84561 Senexin A hydrochloride 1780390-76-2
SHR5428 V79442 SHR5428 SHR5428 is an orally bioavailable, selective non-covalent CDK7 inhibitor (antagonist) with potent CDK7 enzymatic activity (IC50=2.3 nM).
Simurosertib V4595 Simurosertib 1330782-76-7 Simurosertib (formerly known as TAK-931) is a novel, selective and orally bioavailable cycle 7(CDC7, cell division cycle 7-related protein)kinase inhibitor with anticancer activity.
SNS-032 (BMS-387032) V1533 SNS-032 (BMS-387032) 345627-80-7 SNS-032 (also known as BMS-387032; SNS 032; BMS387032; SNS032), a 2-aminothiazole based small-molecule, is a potent and selective inhibitor of CDK2 (cyclin dependent kinase 2) with potential antitumor activity.
SR-4835 V2186 SR-4835 2387704-62-1 SR-4835 (SR4835) is a novel highly selective dual inhibitor of CDK12 and CDK13 with anticancer activity.
SU9516 V1542 SU9516 377090-84-1 SU 9516 (SU-9516; SU9516), a 3-substituted indolinone, is a potent and selectiveCyclin-dependent kinases (CDKs) inhibitor with potential antineoplastic activity.
Tacaciclib V55102 Tacaciclib 2768774-66-7 Tacaciclib is a CDK inhibitor (antagonist) with anti-tumor effects.
Tagtociclib (PF04457845) V41738 Tagtociclib (PF-04457845) 2460249-19-6 PF-07104091 (PF07104091) is a novel and orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2) with potential anticancer activity.
Tanuxiciclib V53286 Tanuxiciclib 1983983-64-7 Tanuxiciclib is a cyclin-dependent kinase (CDK) inhibitor.
Tanuxiciclib trihydrochloride V55079 Tanuxiciclib trihydrochloride 1983984-11-7 Tanuxiciclib triHCl is a cyclin-dependent kinase (CDK) inhibitor.
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TG003 V1548 TG003 719277-26-6 TG003 (TG-003; TG 003) is a novel, potent, selective and ATP-competitive Cdc2-like kinase (Clk) inhibitor with potential anticancer activity.
THZ1 Hydrochloride V76416 THZ1 Hydrochloride THZ1 HCl is a potent and specific covalent CDK7 inhibitor (antagonist) with IC50 of 3.2 nM.
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