CCT018159 is a novel inhibitor of heat shock protein (Hsp) 90 with potential anticancer activity. CCT018159 inhibited human HSP90beta with comparable potency to 17-AAG and with similar ATP-competitive kinetics. The mean cellular GI(50) value of CCT018159 across a panel of human cancer cell lines, including melanoma, was 5.3 mumol/L. CCT018159 caused cell cytostasis associated with a G(1) arrest and induced apoptosis. CCT018159 also inhibited key endothelial and tumor cell functions implicated in invasion and angiogenesis. References: van der Kraan AG, Chai RC, Singh PP, Lang BJ, Xu J, Gillespie MT, Price JT, Quinn JM. HSP90 Inhibitors Enhance Differentiation and Microphthalmia Transcription Factor (MITF) Activity in Osteoclast Progenitors. Biochem J. 2013 Feb 5. [Epub ahead of print] PubMed PMID: 23379601.

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CAS：171009-07-7