Description
7-Cl-O-Nec1 (852391-15-2) is a necrostatin-1 (Cat.# 10-1162) analogue with superior potency (IC50?= 206nM vs 494nM), selectivity and metabolic stability in blocking RIP1.1,2?7-Cl-O-Nec1 shows no off-target inhibition of indolamine-2,3-deoxygenase (IDO) in contrast to Necrostatin-1 (Nec-1).3,4?7-Cl-O-Nec1 showed higher activity in inhibiting necroptosis in Jurkat cells than Necrostatin-1 (EC50?= 210 nM vs. EC50?= 490 nM), no non-specific cytotoxicity at high concentrations (100 μM) and reasonable pharmacokinetic characteristics when used in mice.2?7-Cl-O-Nec1 is recommended for cellular and?in vivo?use over Necrostatin-1.5
Uses
Necrostatin 1s is an inhibitor of indolamine 2,3-deoxygenase. Necrostatin 1s is a neuroprotective with potential therapeutic functions against brain ischemia.
References
1) Degterev?et al. (2005)?Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury; Nat. Chem. Biol.,?1?112
2) Teng?et al. (2005)?Structure-activity relationship of novel necroptosis inhibitors; Bioorg. Med. Chem. Lett.,?15?5039
3) Degterev?et al. (2012)?Activity and specificity of necrostatin-1, small-molecule inhibitor of RIP1 kinase; Cell Death Differ.,?20?366
4) Takahashi?et al. (2012)?Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models; Cell Death Dis.,?3?e437
5) Degterev?et al. (2013)?Addendum: Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury; Nat. Chem. Biol.,?9?192
