Background:

NU6300 is the first covalent ATP-competitive CDK2 inhibitor.IC50 value:Target: CDK2in vitro: NU6300 is a covalent CDK2 inhibitor that illustrates the potential of using vinyl sulfones to mediate irreversible inhibition. NU6300 blocks the inhibitor binding site. The effect was time dependent and relatively slow, with less than 50% reduction of the apparent binding capacity in 20 hr.

[1]. Anscombe E, et al. Identification and Characterization of an Irreversible Inhibitor of CDK2. Chem Biol. 2015 Sep 17;22(9):1159-1164.