Uses
FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively[1].
Biological Activity
FMF-04-159-2 is a specific and potent covalent inhibitor Cyclin-dependent kinase 14 (CDK14) in cells th at targets CDK14 at C218. FMF-04-159-2 reversibly inhibits CDK2, CDK10, and other TAIRE kinases (CDK15, CDK16, CDK17, and CDK18) with comparable potency to each other. It exhibits mild antiproliferative effects.
IC 50
CDK14/Cyclin Y: 39.6 nM (IC
50, in NanoBRET assay); CDK2: 256 nM (IC
50, in NanoBRET assay)
References
[1] Ferguson FM, et al. Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity. Cell Chem Biol. 2019 Mar 11. pii: S2451-9456(19)30070-4. DOI:
10.1016/j.chembiol.2019.02.015