cx-4945-silmitasertib

Description: Silmitasertib (CX-4945; CX4945; CX 4945) is a potent, selective, orally bioavailable small-molecule inhibitor of CK2 (casein kinase 2) with potential anticancer activity. It inhibits CK2 with an IC50 of 1 nM in a cell-free assay, and shows less potency againt Flt3, Pim1 and CDK1 (inactive in cell-based assay). CX-4945 selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2 is a protein kinase overexpressed in a variety of cancer cell types and is correlated with malignant transformation, tumor growth and survival.

References: Cancer Res. 2010 Dec 15; 70(24):10288-98; J Med Chem. 2011 Jan 27; 54(2):635-54.