CDK

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 2.7.11.22) 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.

Items 1 to 30 of 34 total

per page
Page:
  1. 1
  2. 2
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
4071 AMG-925 Potent, selective, and orally available FLT3/CDK4 dual inhibitor Inquire
1539 AT 7519 mesylate CDK inhibitor €80.00
3800 AZD4573 Inhibitor of CDK9 Inquire
1966 AZD5438 CDK inhibitor (1, 2, and 9 specific) €80.00
3935 BAY-1251152 Potent and highly selective CDK9/P-TEFb inhibitor Inquire
3228 CDK inhibitor CR8 Potent CDK inhibitor (1, 2, 5, 7, and 9 specific) €130.00
3756 CT-7001 dihydrochloride Specific CDK7 inhibitor Inquire
1776 Dinaciclib CDK inhibitor (1, 2, 5, and 9 specific) €90.00
3525 ETP-47799 Potent CDK8/CDK19 inhibitor  Recently added €90.00
3667 Homoharringtonine Protein synthesis inhibitor; Binds the 60S ribosomal subunit €100.00
3730 KB-0742 dihydrochloride Orally bioavailable, potent and selective CDK9 inhibitor Inquire
3029 LDC000067 Potent, highly specific, ATP-competitive CDK9 inhibitor €110.00
2273 LEE 011 Orally bioavailable and highly selective small-molecule inhibitor of CDK4/6 €80.00
3283 LY2857785 Highly potent, selective, reversible and ATP-competitive CDK9 inhibitor €180.00
1243 NSC 625987 CDK4 inhibitor €95.00
3876 OTS-964 TOPK (T–lymphokine-activated killer cell–originated protein kinase) inhibitor Inquire
4171 OTS514 Highly potent TOPK inhibitor €130.00
4097 OTS964 hydrochloride TOPK (T–lymphokine-activated killer cell–originated protein kinase) inhibitor €120.00
2052 Palbociclib isethionate Orally active cyclin-dependent kinase (CDK4/6) inhibitor €125.00
1505 PD0332991 hydrochloride CDK4 and CDK6 inhibitor €85.00
3693 PF-06873600 CDK inhibitor (4, 6, and 8 specific) Inquire
3753 PF-07104091 Specific CDK2 inhibitor €140.00
3762 PF-07220060 Orally bioavailable and CDK4-Specific Inhibitor 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
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

Items 1 to 30 of 34 total

per page
Page:
  1. 1
  2. 2
Please wait...