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GSK 2982772
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C20H19N5O3
- MW: 377.4
Description
GSK2982772 potently binds to RIP1 with exquisite kinase specificity (IC50 value of 1.0 nM; ADP-Glo activity assay) and has excellent activity in blocking many TNF-dependent cellular responses (IC50 value of 6.3 nM; human monocytic U937 cellular assay). The inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants. First-in-class RIP1 inhibitor to enter clinical trials for psoriasis, rheumatoid arthritis, and ulcerative colitis.
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 |
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