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Beschreibung

A cell-permeable pyrazoloresorcinol compound that inhibits HSP90 ATPase activity (IC50 = 3.2 µ,M and 6.6 µ,M against human HSP90beta and yeast HSP90, respectively) by targeting the enzyme's N-terminal ATP binding site. It exhibits no detectable effects against human Hsp70 or topoisomerase II even at concentrations as high as 100 µ,M and inhibits a panel of 20 commonly studied kinases only at much higher concentrations. Unlike 17-AAG (Cat. No. 100068), the antitumor activity of CCT018159 is not affected by the expression of NQ01/DT-diaphorase or P-glycoprotein.