MFH290 (MFH-290; MFH 290) is a highly selective cysteine (Cys)-targeted, irreversible/covalent inhibitor of CDK12/13 with potential antitumor activity. It forms a covalent bond with Cys-1039 of CDK12, and exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.

纯度：≥98%

CAS：2088715-91-5