Necrostatin-2 - RIP kinase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENecrostatin 2Cat. No.: HY-14622CAS No.: 852391-19-6分式: CHClNO分量: 277.71作靶点: RIP kinase作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (360.09 mM)* means soluble, but

2、 saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.6009 mL 18.0044 mL 36.0088 mL5 mM 0.7202 mL 3.6009 mL 7.2018 mL10 mM 0.3601 mL 1.8004 mL 3.6009 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备

3、液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.00 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.00 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Mole

4、cules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (9.00 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Necrostatin 2种有效的程序性坏死 (necroptosis) 抑制剂。作于TNF-处理的FADD缺陷型Jurkat T细胞，抑制程序性坏死，EC50 为 0.05 M。Necrostatin 2 为 RIPK1 抑制剂。IC50 & Target Necroptosis 1, RIPK1 4体外研究 Evaluation of necroptosis inhibitory activity is

5、 performed using a FADD-deficient variant of human Jurkat Tcells treated with TNF-. Utilizing these conditions the cells efficiently undergo necroptosis, which iscompletely and selectively inhibited by Necrostatin 2 (EC50=50 nM). Necrostatin 2 shows activity in a broadrange of necroptosis cellular s

6、ystems 1. Necrostatin 2 at 30 M completely protects L929 cells from TNF-induced necroptosis. In addition to TNF-, the pan-caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone (zVAD.fmk) has also been found to induce necrosis in L929 cells, which is efficientlyinhibited by Necrosta

7、tin 2 2. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated withTNF- is 0.05 M 3.PROTOCOLKinase Assay 2 Evaluation of necroptosis inhibitory activity is performed using an FADD-deficient variant of human Jurkat Tcells treated for 24 h with TNF-. Under these conditions the ce

8、lls underwent necroptosis (the DMSO controlhad 40% viability), which is inhibited by Necrostatin 2 (EC50=0.210.2 M) as a positive control. For EC50value determinations, cells are treated with 10 ng/mL human TNF- in the presence of increasingconcentrations of test compounds (0.029, 0.058, 0.12, 0.23,

9、 0.46, 0.93, 1.9, 3.7, 11.1, 33, and 100 M) induplicate for 24 h followed by ATP-based viability assessment. EC50 valuesSD are determined from atleast two independent experiments 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 L929 cells

10、(100000 cells/mL, 100 L/well in a 96-well plate) are treated with 10 ng/mL human TNF- or 100 M zVAD.fmk in the presence of DMSO (control), 30 M Necrostatin 2, or 8for 24 h at 37C in a humidifiedincubator with 5% CO2 followed by ATP-based viability assessment as described in the previous experiment.S

11、tock solutions (30 mM) in DMSO are initially prepared and then diluted with DMSO to give testing solutions.Each sample is done in duplicate. The final DMSO concentration is 0.5%. Cell viability values are adjusted toaccount for nonspecific toxicity, which in most cases is 2.MCE has not independently

12、 confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 FEBS Open Bio. 2018 Dec.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Teng X, et al. Structure-activity relationship study of 1,2,3thiadiazole ne

13、croptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec15;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):5039-44.4. Takahashi N, et al. Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models.Cell Death Dis. 2012 Nov 29;3:e