GSK620

• CAT Number: I028391
• CAS Number: 2088410-46-0
• Molecular Formula: C18H19N3O3
• Molecular Weight: 325.36
• Purity: ≥95%
• Synonyms: 1-benzyl-5-N-cyclopropyl-3-N-methyl-2-oxopyridine-3,5-dicarboxamide
• InChI: InChI=1S/C18H19N3O3/c1-19-17(23)15-9-13(16(22)20-14-7-8-14)11-21(18(15)24)10-12-5-3-2-4-6-12/h2-6,9,11,14H,7-8,10H2,1H3,(H,19,23)(H,20,22)
• InChIKey: QZZCUOVXHPAQRQ-UHFFFAOYSA-N
• SMILES: CNC(=O)C1=CC(=CN(C1=O)CC2=CC=CC=C2)C(=O)NC3CC3

GSK620（Cat No.:I028391）is a selective, orally bioavailable small-molecule inhibitor that targets the BD2 domains of BET (bromodomain and extra-terminal) proteins, including BRD2, BRD3, BRD4, and BRDT. It exhibits approximately 200-fold selectivity for BD2 over BD1, making it a valuable tool for dissecting BET domain-specific functions. GSK620 effectively suppresses inflammatory cytokine production, such as MCP-1, in LPS-stimulated human whole blood. In preclinical models like collagen-induced arthritis, it reduces disease severity in a dose-dependent manner. With good solubility and pharmacokinetics, GSK620 is widely used in inflammation and epigenetic regulation research.

Reference

[1]. Seal JT, et al. The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor. J Med Chem. 2020;63(17):9093-9126.
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