Necrosulfonamide是一种坏死性凋亡抑制剂,选择性靶向混合谱系激酶结构域样蛋白(MLKL),阻止MLKL-RIP1-RIP3坏死小体复合物与下游效应分子的相互作用。MLKL是RIP3在坏死诱导过程中关键的底物。(Necrosulfonamide具有人源MLKL特异性,不能靶向抑制鼠源MLKL,不能抑制鼠源细胞和小鼠中MLKL依赖的坏死性凋亡。)
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描述 | Necrosulfonamide functions as an inhibitor of necroptosis by selectively inhibiting the mixed lineage kinase domain-like protein (MLKL). It obstructs the interaction between the MLKL-RIP1-RIP3 necrosome complex and its subsequent effectors. During necrosis initiation, MLKL is an essential target of RIP3. Necrosulfonamide acts downstream of RIP3 activation to specifically impede necrosis. It hinders necrosis driven by MLKL by inhibiting the functionality of its N-terminal CC domain[1]. |
体外研究 | Necrosulfonamide (NSA) effectively protects human cells from TNF-a, Smac mimetic (LCL161), z-VAD-fmk-triggered necroptosis, but not mouse cells. The reason for the species specificity of necrosulfonamide is that the cysteine at residue 86 in human MLKL that is covalently modified by necrosulfonamide is replaced by a tryptophan residue in mouse MLKL[1]. NSA blocks phospho-MLKL targeting to membranes and attenuats liposome leakage without preventing MLKL phosphorylation[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.83mL 2.17mL 1.08mL |
21.67mL 4.33mL 2.17mL |
CAS号 | 1360614-48-7 |
分子式 | C18H15N5O6S2 |
分子量 | 461.472 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 30 mg/mL(65.01 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |