Synonyms: GSK 2795039; GSK-2795039; N-(1-Isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide
Molecular Formula: C23H26N6O2S
Molecular Weight: 450.56
Linear Structural Formula: C23H26N6O2S
MDL Number: MFCD30489720
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: GSK2795039 is a non-cytotoxic (100 muM, 24 hrs, HEK293), NADPH-competitive, potent and selective NOX2 inhibitor (IC50/[NADPH] = 447 nM/25 muM, 2.29 muM/1 mM by NADPH depletion measurement; eNOS & NOX1/3/4/5 IC50 >100 muM, PKCB II IC50 >25 muM, xanthine oxidase IC50 = 28.8 muM). GSK2795039 inhibits PMA-induced reactive oxygen species (ROS) production in cultures (IC50 = 182 nM; HL60) and exhibits in vivo efficacy against complete Freund's adjuvant-induced paw inflammation (ED50 = 2 mg/kg, ED100 = 100 mg/kg ip.) as well as cerulein-induced acute pancreatitis (ED50 = 100 mg/kg ip.) in mice.