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GSK481
- GSK'481
- Soluble in DMSO
- MF: C21H19N3O4
- MW: 377.39
Description
GSK481 (GSK'481) is a highly potent and selective inhibitor of Receptor-interacting serine/threonine-protein kinase 1 (RIPK1 or RIP1) with a biochemical IC50 value of 1.3 nM against RIPK1. It blocks the autophosphorylation of Ser166 on human wild-type RIP1 with an IC50 of 2.8 nM. It exhibits a remarkable specificity over 450 alternative kinases. GSK481 functions as a critical research tool to block programmed necrotic cell death (necroptosis) and pathways driving tumor necrosis factor (TNF)-mediated inflammation.
RIP1 kinase pharmacology is central to inflammation signaling. GSK481 supports mechanistic studies of RIP1 kinase and RIP1 inhibition in biochemical, cellular and disease-model assays.
Key Features
- Potent and selective RIP1 inhibitor
- Inhibits RIP1 (IC50: 1.3 nM) and human Ser166 autophosphorylation (IC50: 2.8 nM)
- Highly selective over 450+ alternative kinases
- Blocks necroptosis and TNF-mediated inflammatory pathways
Applications
- RIP1 kinase pharmacology and target-validation studies
- RIP1 kinase pathway and signaling assays
- Disease-model research related to inflammation
- Kinase signaling, phosphorylation and pathway-inhibition assays
More Information
| Parent CAS No. | 1622849-58-4 |
|---|---|
| Chemical Name | (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide |
| MFCD | N.A. |
| Short Description | RIP1 kinase inhibitor |
References
- PA Harris 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.
- P Geserick et al. Absence of RIPK3 predicts necroptosis resistance in malignant melanoma. Cell Death Dis. 2015 Sep 10;6:e1884.
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