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GSK481

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Chemical Structure| 1622849-58-4 同义名 : -
CAS号 : 1622849-58-4
货号 : A135126
分子式 : C21H19N3O4
纯度 : 99%+
分子量 : 377.393
MDL号 : MFCD30343843
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(92.74 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • TNF-α
描述 GSK481, recognized for its high potency, selectivity, and specificity, acts as an inhibitor of receptor interacting protein 1 (RIP1) kinase, demonstrating an IC50 value of 1.3 nM. It effectively hampers Ser166 phosphorylation in human RIP1, with an IC50 of 2.8 nM. In cellular assays involving U937 cells, GSK481 maintains its efficacy, reflected by an IC50 of 10 nM[1]. In experiments using Jurkat cells, when treated with GSK481 at a concentration of 300 nM for 2 hours, there is a notable prevention of RIP3 up-regulation, which is typically triggered by TNFa and shikonin. This outcome suggests that necroptosis is indeed initiated by these compounds[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.26mL

13.25mL

2.65mL

1.32mL

26.50mL

5.30mL

2.65mL
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.