CMPD 7 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.
CMPD 7 is a highly selective CDK12 inhibitor profiled across a panel of 352 kinases at 0.1 µM. CMPD 7 shows potent inhibition of phosphorylation of Ser2 on the CTD repeat domain of RNA Pol II as well as growth inhibition of OV90 cells and acute cytotoxicity to THP1 cells[1].
[1]. Johannes JW, et al. Structure-Based Design of Selective Noncovalent CDK12 Inhibitors. ChemMedChem. 2018 Feb 6;13(3):231-235.