Cancer

In vitro and cell culture studies identified an aminothiazole-based negative allosteric modulator (NAM) of CSNK2 that could help treat renal cell carcinoma (RCC). Chemical synthesis and in vitro testing of aminothiazole analogs yielded a compound that bound an allosteric site on CSNK2 with a K_i of 0.18 μM and inhibited CSNK2 activity with an IC₅₀ of 0.6 μM. In a human RCC cell line, the compound inhibited growth with greater potency than the CSNK2 inhibitor CX-4945 (EC50 values of 5 and 6 μM, respectively). Next steps could include testing the compound in mouse models of RCC.

Senhwa Biosciences Inc. has CX-4945, an oral protein kinase CSNK2 inhibitor, in Phase II testing for biliary cancer...