Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Necrosulfonamide ((E)-Necrosulfonamide) 是一种坏死性凋亡抑制剂,通过选择性靶向(MLKL),可阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。MLKL 是诱导坏死过程中 RIP3 的重要底物。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 198 | 现货 | ||
5 mg | ¥ 441 | 现货 | ||
10 mg | ¥ 579 | 现货 | ||
25 mg | ¥ 1,210 | 现货 | ||
50 mg | ¥ 1,830 | 现货 | ||
100 mg | ¥ 3,320 | 现货 | ||
500 mg | ¥ 7,290 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 441 | 现货 |
产品描述 | (E)-Necrosulfonamide ((E)-Necrosulfonamide) is an inhibitor of necroptosis. Blocks mixed lineage kinase domain-like protein (MLKL), a critical substrate of receptor-interacting serine-threonine kinase 3 (RIP3) during necrosis. Prevents MLKL-RIP1-RIP3 necrosome complex from interacting with downstream necrosis effectors. Binds and inhibits gasdermin D. Inhibits pyroptosis. |
体外活性 | Necrosulfonamide inhibits MLKL-mediated Necrosis by blocking its N-terminal CC domain function. It blocks necrosis downstream of RIP3 activation. Necrosulfonamide has no effect on apoptosis induced by TNF-α plus Smac mimetic in non-RIP3-expressing Panc-1 cells, even at 5 μM concentration. Necrosulfonamide efficiently blocks necrosis in human cells, 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(mixed lineage kinase domain-like protein)[2]. |
激酶实验 | PRMT Biochemical Assays: A scintillation proximity assay (SPA) is used for assessing the effect of test compounds on inhibiting the methyl transfer reaction catalyzed by PRMTs. In brief, the tritiated S-adenosyl-L-methionine (3H-SAM) is used as the donor of methyl group. The (3H) methylated biotin labeled peptide is captured in a streptavidin/scintillant-coated microplate, which brings the incorporated 3H-methyl and the scintillant to close proximity resulting in light emission that is quantified by tracing the radioactivity signal (counts per minute) as measured by a TopCount NXT Microplate Scintillation and Luminescence Counter. When necessary, nontritiated SAM is used to supplement the reactions. The IC50 values are determined under balanced conditions at Km concentrations of both substrate and cofactor by titration of test compounds in the reaction mixture. |
细胞实验 | Necrosis inhibitors induce diverse effects on MLKL phosphorylation. HT-29 cells are treated with T/S/Z with or without necrosis inhibitors for 12 hr or 8 hr. The number of dead cells is determined by measuring released protease activity in culture medium. The whole-cell extracts are prepared and analyzed by western blotting. The final concentrations of 10 μM necrostatin-1 or 1 μM necrosulfonamide are used to block necrosis. (Only for Reference) |
别名 | (E)-Necrosulfonamide |
分子量 | 461.47 |
分子式 | C18H15N5O6S2 |
CAS No. | 1360614-48-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9.2 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.167 mL | 10.8349 mL | 21.6699 mL | 54.1747 mL |
5 mM | 0.4334 mL | 2.167 mL | 4.334 mL | 10.8349 mL | |
10 mM | 0.2167 mL | 1.0835 mL | 2.167 mL | 5.4175 mL | |
20 mM | 0.1083 mL | 0.5417 mL | 1.0835 mL | 2.7087 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Necrosulfonamide 1360614-48-7 MAPK MLK (E)-Necrosulfonamide formation necrosis necrosome substrate RIP3 Inhibitor inhibit complex Mixed Lineage Kinase MLKs inhibitor