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.
| 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 | Recently added | €130.00 |
| 4097 | OTS964 hydrochloride | TOPK (T–lymphokine-activated killer cell–originated protein kinase) inhibitor | Recently added | €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 | |