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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
If you know of a relevant reference for EC 144 please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses EC 144 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: EC 144, supplier, EC144, high, affinity, potent, selective, HSP90, heat, shock, proteins, inhibitors, inhibits, her-2, antitumor, orally, available, brain, penetrant, Tocris Bioscience, Hsp90 Inhibitor products
Find multiple products by catalog number
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.