CCT-018159

CCT-018159 is a novel, synthetic small molecule inhibitor of heat shock protein 90 (Hsp90) ATPase activity. It belongs to the diaryl pyrazole resorcinol class and acts as an ATP-competitive inhibitor, selectively targeting Hsp90 over related proteins such as Hsp72 and topoisomerase II. The compound inhibits proliferation of various human cancer cell lines, including colon tumor cells (HCT116), induces G1 cell cycle arrest, upregulates Hsp70 expression, and downregulates c-Raf and cdk4. Its antitumor activity is independent of NQO1/DT-diaphorase or P-glycoprotein expression. Discovered by high-throughput screening at the Centre for Cancer Therapeutics (CCT) at The Institute for Cancer Research in London, it has been developed primarily for potential anticancer applications but remains in preclinical development[1][3][6][9].