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Background Information:
GSK2982772 is an oral, potent and selective RIP1 (Receptor Interacting Protein 1) Kinase inhibitor, a First-in-class to enter clinical trials for psoriasis, rheumatoid arthritis, and ulcerative colitis. It 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). It was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants.
Reference:
1. PA Harris, et al, Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261.
APIM050035: GSK2982772
CAS No.: 1622848-92-3.
Molecular Formula: C20H19N5O3?0.2H2O.
Molecular Weight: 381.0.
Purity: 99.9% chemical and optical purity (by achiral and chiral HPLCs).
QC: Achiral and Chiral HPLCs, 1H-NMR and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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