SML2770
GSK2795039
≥98% (HPLC), NOX2 inhibitor, powder
Synonym(s):
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
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About This Item
Empirical Formula (Hill Notation):
C23H26N6O2S
CAS Number:
Molecular Weight:
450.56
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Product Name
GSK2795039, ≥98% (HPLC)
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
O=S(NC1=C2C(N(C(C)C)C=C2C3=CC4=C(C=C3)CCN4C)=NC=C1)(C5=NN(C)C=C5)=O
InChI key
FMWVTCZKCXPKFW-UHFFFAOYSA-N
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
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