Necrostatin 2

"目录号: HY-14622 ee.: 99.20%

Apoptosis-

Necrostatin 2 是一种有效的程序性坏死 (necroptosis) 抑制剂。作用于TNF-α处理的FADD缺陷型Jurkat T细胞，抑制程序性坏死，EC50为 0.05 μM。

TNF-alpha

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生物活性

Description

Necrostatin 2 is a potentnecroptosisinhibitor.EC50for inhibition of necroptosis in FADD-deficient Jurkat T cells treated withTNF-αis 0.05 μM.

IC50& Target

Necroptosis[1]

In Vitro

Evaluation of necroptosis inhibitory activity is performed using a FADD-deficient variant of human Jurkat T cells treated with TNF-α. Utilizing these conditions the cells efficiently undergo necroptosis, which is completely and selectively inhibited by Necrostatin 2 (EC50=50 nM). Necrostatin 2 shows activity in a broad range of necroptosis cellular systems[1]. Necrostatin 2 at 30 μM completely protects L929 cells from TNF-α-induced necroptosis. In addition to TNF-α, the pan-caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone (zVAD.fmk) has also been found to induce necrosis in L929 cells, which is efficiently inhibited by Necrostatin 2[2]. EC50for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM[3].

References

[1].Teng X, et al. Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836-40.

[2].Jagtap PG, et al. Structure-activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 2007 Apr 19;50(8):1886-95.

[3].Teng X, et al. Structure-activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5039-44.