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
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
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