| Bioactivity | 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[1]. | ||||||||||||
| Target | IC50: 1.3 nM (RIP1), 2.8 nM (Ser166 phosphorylation in wild-type human RIP1) | ||||||||||||
| Invitro | 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[2]. Apoptosis Analysis[2] Cell Line: | ||||||||||||
| In Vivo | GSK481 inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse[1]. | ||||||||||||
| Name | GSK481 | ||||||||||||
| CAS | 1622849-58-4 | ||||||||||||
| Formula | C21H19N3O4 | ||||||||||||
| Molar Mass | 377.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |