Cat. No. 4701
Chemical Name: 5-[2-Amino-4-chloro-7-[(4-methoxy-3
Biological ActivityHigh affinity, potent and selective Hsp90 inhibitor (Ki = 0.2 nM and IC50 = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (Ki values are 61 and 255 nM respectively) and has no effect (IC50 >10 μM) against a panel of 285 kinases. Degrades Her-2 in MCF-7 breast cancer cells (EC50 = 14 nM). Blocks tumor growth and induces partial tumor regression in an N87 gastric tumor mouse model. Also inhibits LPS-induced TNFα release in an LPS shock mouse model and suppresses disease development in a rat model of collagen-induced arthritis. Exhibits <20-fold efficacy over BIIB 021 (Cat. No. 4608) in mice. Orally available and brain penetrant.
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Shi et al (2012) EC144 is a potent inhibitor of the heat shock protein 90. J.Med.Chem. 55 7786. PMID: 22938030.
Yun et al (2011) EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity. J.Immunol. 186 563. PMID: 21131419.
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