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CCT 018159 is a cell-permeable pyrazoloresorcinol compound that inhibits heat shock protein 90 (Hsp90) ATPase activity (IC50 = 3.2 muM and 6.6 muM against human HSP 90 beta and yeast Hsp90, respectively) by targeting the enzyme′s N-terminal ATP binding site. CCT 018159 exhibits no detectable effects against human HSP 70 or topoisomerase II even at concentrations as high as 100 μM and inhibits a panel of 20 studied kinases only at much higher concentrations. Unlike 17-AAG, the antitumor activity of CCT 018159 is not affected by the expression of NQ01/DT-diaphorase or P-glycoprotein. The mean cellular GI value of CCT 018159 across a panel of human cancer cell lines, including melanoma, was 5.3 mumol/L, and it caused cell cytostasis associated with a G arrest and induced apoptosis. Additionally, CCT 018159 inhibited essential endothelial and tumor cell functions related to invasion and angiogenesis.
Ordering Information
Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CCT 018159, 5 mg | sc-202526 | 5 mg | $91.00 |