EC 144

Biological Activity

EC 144 is a high affinity, potent and selective Hsp90 inhibitor (K_i = 0.2 nM and IC₅₀ = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (K_i 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. EC144 is a potent inhibitor of the heat shock protein 90.
   Shi et al.
   J.Med.Chem., 2012;55:7786
2. EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity.
   Yun et al.
   J.Immunol., 2011;186:563

Product Datasheets