Necrostatin-2 - RIP kinase 抑制劑 - 生命科學(xué)試劑 - 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作靶點: RIP kinase作通路: Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (360.09 mM)* means soluble, but

2、 saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備

3、液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.00 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.00 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Mole

4、cules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (9.00 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Necrostatin 2種有效的程序性壞死 (necroptosis) 抑制劑。作于TNF-處理的FADD缺陷型Jurkat T細胞，抑制程序性壞死，EC50 為 0.05 M。Necrostatin 2 為 RIPK1 抑制劑。IC50 & Target Necroptosis 1, RIPK1 4體外研究 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.戶使本產(chǎn)品發(fā)表的科研獻 FEBS Open Bio. 2018 Dec.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師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