货号	规格	价格	上海	北京	珠海	重庆	武汉
S81378-5mg买3赠1	99.80%	￥350.00 S81378-5mg ￥350.00 现货（买3赠1）	6 6	-	-	-	-
S81378-10mg促销	99.80%	￥450.00 ￥360.00 S81378-10mg ￥360.00 现货	7 7	-	-	-	-
S81378-25mg促销	99.80%	￥550.00 ￥440.00 S81378-25mg ￥440.00 现货	5 0 5	-	-	-	-
S81378-100mg促销	≥98%	￥1990.00 ￥1590.00 S81378-100mg ￥1590.00 2-3天	0 货期：2-3天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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浓度

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分子摩尔量

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GSK481

5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)