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GSK 2982772
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C20H19N5O3
- MW: 377.4
Description
GSK2982772 is a potent and highly selective inhibitor of receptor-interacting protein kinase 1 (RIPK1/RIP1). It inhibits RIPK1 with an IC50 of 1.0 nM in an ADP-Glo biochemical assay and blocks TNF-dependent responses in human U937 monocytic cells with an IC50 of 6.3 nM. RIPK1 inhibition suppresses kinase-dependent inflammatory signaling and necroptotic cell death while preserving RIPK1 scaffold functions.
GSK2982772 reduces spontaneous cytokine production in human ulcerative-colitis tissue explants and was the first RIPK1 inhibitor to enter clinical studies for chronic inflammatory diseases. The compound is markedly less potent against mouse RIPK1 than human RIPK1, an important consideration when selecting in vivo models. It is a valuable probe for human TNF–RIPK1 signaling, necroptosis, and cytokine-driven inflammation.
Key Features
- Potent and highly selective RIPK1 kinase inhibitor
- IC50: 1.0 nM in an ADP-Glo biochemical assay
- IC50: 6.3 nM in a human U937 cellular assay
- Blocks TNF-dependent inflammatory and necroptotic responses
- Displays substantial human-to-mouse potency differences
Applications
- RIPK1 kinase pharmacology
- TNF signaling and cytokine production
- Necroptosis and regulated cell-death research
- Ulcerative colitis and inflammatory-disease models
- Species-selectivity and translational pharmacology
More Information
| Parent CAS No. | 1622848-92-3 |
|---|---|
| Chemical Name | (S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1H-1,2,4-triazole-3-carboxamide |
| SMILES | C1C=C2OC[C@H](NC(=O)C3N=C(CC4C=CC=CC=4)NN=3)C(=O)N(C)C2=CC=1 |&1:5,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C20H19N5O3/c1-25-15-9-5-6-10-16(15)28-12-14(20(25)27)21-19(26)18-22-17(23-24-18)11-13-7-3-2-4-8-13/h2-10,14H,11-12H2,1H3,(H,21,26)(H,22,23,24)/t14-/m0/s1 |
| InChiKey | LYPAFUINURXJSG-AWEZNQCLSA-N |
| CID | 77108121 |
| Short Description | RIP1 inhibitor |
