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SML2770

Sigma-Aldrich

GSK2795039

≥98% (HPLC)

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:
1415925-18-6
Molecular Weight:
450.56
MDL number:
MFCD30489720
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

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 Code

11 - Combustible Solids

WGK

WGK 3

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Certificates of Analysis (COA)

Lot/Batch Number
0000402772
0000402771
0000396761
0000396761
0000402772

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