GSK2795039，1MG，SML2770-1MG，Sigma

Biochem/physiol Actions

GSK2795039 is a non-cytotoxic (100 μM, 24 hrs, HEK293), NADPH-competitive, potent and selective NOX2 inhibitor (IC₅₀/[NADPH] = 447 nM/25 μM, 2.29 μM/1 mM by NADPH depletion measurement; eNOS & NOX1/3/4/5 IC₅₀ >100 μM, PKCB II IC₅₀ >25 μM, xanthine oxidase IC₅₀ = 28.8 μM). 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.
NADPH-competitive, potent and selective NOX2 inhibitor with in vitro and in vivo efficacy against NOX2-mediated ROS production and inflammation.