Chemical Name: 6-(2-Aminophenoxy)-1,2-benzisothiazol-3-amine dihydrochloride
Biological ActivityTLR4 inhibitor. Inhibits LPS-induced NF-κB activation in HEK293 cells (IC50 = 2.4 μg/mL). Also inhibits LPS-induced cytokine production and procoagulant effects in PBMCs and HUVECs. Prolongs survival in a mouse septic shock model.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Toll-like receptor 4 signal transduction inhibitor, M62812, suppresses endothelial cell and leukocyte activation and prevents lethal septic shock in mice.
Nakamura M, Shimizu Y, Sato Y, Miyazaki Y, Satoh T, Mizuno M, Kato Y, Hosaka Y, Furusako S
Eur. J. Pharmacol., 2007;569(3):237-43.
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We were interested in looking at LPS TLR4 mediated signaling and were hoping to use this to block this.