MPC-3100

MPC-3100 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 0.14 µM in a fluorescence polarization assay). It inhibits proliferation of a variety of cancer cell lines, including colon, prostate, ovarian, gastric, and breast cancer cells (IC50s = 0.2-0.55 µM), as well as MV4-11 leukemia, A549 non-small cell lung cancer (NSCLC), NCI H69 SCLC, and multidrug-resistant NCI/ADR-RES cells (IC50s = 0.25, 0.77, 0.15, and 4.3 µM, respectively). MPC-3100 induces degradation of the Hsp90 client proteins Akt and HER2 (IC50s = 0.1-0.5 µM) and a compensatory Hsp70 response in NCI N87, HCT116, and DU145...