The cell cycle, consisting of four distinct phases (G1, S, G2, and M) is controlled by numerous mechanisms ensuring correct cell division. Cyclin-dependent kinases (CDKs; EC are a family of protein kinases first discovered for their role in regulating the cell cycle[1]. Their kinase activity requires the binding of a regulatory cyclin subunit, upon which CDKs phosphorylate their substrates on serine and threonine  residues. Since cyclins are synthesized and destroyed at specific times during the cell cycle, CDK kinase activity is regulated in a timely manner. Tumor associated mutations frequently deregulate certain CDK–cyclin complexes, resulting in either continued proliferation or unscheduled re-entry into the cell cycle, two properties characteristic of most human tumor cells[2],[3]. If it is possible to selectively interrupt the cell cycle regulation in cancer cells by interfering with CDK action, the cell will die. Therefore, the development of CDK inhibitors (CKIs) is of great interest.

[1] The cell cycle: a review of regulation, deregulation and therapeutic targets in cancer. K. Vermeulen, D.R. Van Bockstaele , Z.N. Berneman. Cell Prolif. 2003, 36, 131–149.
[2] Cell cycle, CDKs and cancer: a changing paradigm. M.Malumbres, M.Barbacid. Nature Reviews Cancer 2009, 9, 153-166.
[3] CDK Inhibitors: Cell Cycle Regulators and Beyond. Develop. Cell 2008, 14, 159-169.

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Axon ID Name Description From price
1892 1-NM-PP1 Potent tyrosine kinase inhibitor (TKI) of multiple targets (Src, Fyn, Abl, CDK, Trk) €95.00
1539 AT 7519 mesylate CDK inhibitor €80.00
1966 AZD 5438 CDK inhibitor (1, 2, and 9 specific) €80.00
3228 CDK inhibitor CR8 Potent CDK inhibitor (1, 2, 5, 7, and 9 specific) €130.00
3667 Homoharringtonine Protein synthesis inhibitor; Binds the 60S ribosomal subunit  Recently added €100.00
2273 LEE 011 Orally bioavailable and highly selective small-molecule inhibitor of CDK4/6 €80.00
3535 MS140 Potent and selective CDK4/6 inhibitor; PROTAC €100.00
1243 NSC 625987 CDK4 inhibitor €95.00
2052 Palbociclib isethionate Orally active cyclin-dependent kinase (CDK4/6) inhibitor €125.00
1505 PD 0332991 hydrochloride CDK4 and CDK6 inhibitor €85.00
3693 PF-06873600 CDK inhibitor (4, 6, and 8 specific)  Recently added Inquire
2690 PHA-767491 Dual CDC7/CDK9 kinase inhibitor €95.00
1983 R 547 CDK inhibitor (1, 2, and 4 specific) €95.00
1530 RO 3306 CDK1 inhibitor €80.00
1776 SCH 727965 CDK inhibitor (1, 2, 5, and 9 specific) €90.00
1614 SNS 032 CDK inhibitor (2, 7 and 9 specific) €85.00
3184 SR-4835 Potent, highly selective and orally bioavailable dual CDK12/CDK13 inhibitor €130.00
3560 THZ1 Covalent CDK7 inhibitor €60.00
3561 THZ1 dihydrochloride Covalent CDK7 inhibitor  Recently added €110.00
3402 THZ531 First-in-class, potent, selective, covalent CDK12/CDK13 inhibitor €130.00

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