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GSK2982772 is an ATP-competitive inhibitor of receptor-interacting protein-1 (RIP1) kinase (RIPK1) with an IC50 of 16 nM. It is able to inhibit a variety of TNF-dependent cellular responses with good kinase specificity and cellular activity.
Brand: BCM
Target: RIP kinase
Signaling Pathways: Apoptosis; NF-κB
In Vitro: GSK2982772 ?potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking many TNF-dependent cellular responses.?Highlighting its potential as a novel anti-inflammatory agent, the inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants.
pKa: 8.80±0.40(Predicted)
Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.
GHS: GHS07
Isomeric SMILES: CN1C2=CC=CC=C2OC[C@@H](C1=O)NC(=O)C3=NNC(=N3)CC4=CC=CC=C4
InChIKey: LYPAFUINURXJSG-AWEZNQCLSA-N
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
Attribute [CAS No.] 1622848-92-3 [Formula] C20H19N5O3 [Molecular] 377.39656 [Chem Name] 5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide [Storage] Sealed in dry. Store in freezer, under -20°C [Synonym] GSK2982772 [MDL No.] MFCD30489467 [Form] Off-white solid
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