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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);RIPkinase

• 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 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *