Merck, 385920-5MG, HSP90 Inhibitor, CCT018159

General description
A cell-permeable pyrazoloresorcinol compound that inhibits HSP90 ATPase activity (IC₅₀ = 3.2 µM and 6.6 µM against human HSP90β 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 µM 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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solution are stable for up to 3 months at -20°C.
Other Notes
Hardcastle, A., et al. 2007. Mol. Cancer Ther.6, 1112.
Sharp, S.Y., et al. 2007. Cancer Res.67, 2206.
Smith, N.F., et al. 2006. Mol. Cancer Ther.5, 1628.
Dymock, B.W., et al. 2005. J. Med. Chem.48, 4212.
Cheung, K.M., et al. 2005. Bioorg. Med. Chem. Lett.15, 3338.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)