S81378 |
GSK481 |
| 源叶(MedMol) | 98% |
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- 产品描述： GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM
- 靶点： IC50: 1.3 nM (RIP1), 2.8 nM (Ser166 phosphorylation in wild-type human RIP1)
- 体外研究： GSK481 (300 nM; 2 hours; Jurkat cells) abrogates the RIP3 up-regulation induces by both TNFa and shikonin in live and dead cells, indicating that necroptosis is in fact induced by both agents. Apoptosis Analysis Cell Line: Jurkat cells Concentration: 300 nM Incubation Time: 2 hours Result: Increased levels of detectable apoptosis induced by TNFa and shikonin.
- 体内研究： GSK481 inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse
- 参考文献：
1. Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78. 2. Lee HL, et al. Simultaneous flow cytometric immunophenotyping of necroptosis, apoptosis and RIP1-dependent apoptosis. Methods. 2018 Feb 1;134-135:56-66.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.65 ml 13.249 ml 26.498 ml 5 mM 0.53 ml 2.65 ml 5.3 ml 10 mM 0.265 ml 1.325 ml 2.65 ml 50 mM 0.053 ml 0.265 ml 0.53 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
