SML2770
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:
Molecular Weight:
450.56
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
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
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.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Swenja Kröller-Schön et al.
European heart journal, 39(38), 3528-3539 (2018-06-16)
Aircraft noise causes endothelial dysfunction, oxidative stress, and inflammation. Transportation noise increases the incidence of coronary artery disease, hypertension, and stroke. The underlying mechanisms are not well understood. Herein, we investigated effects of phagocyte-type NADPH oxidase (Nox2) knockout and different
Shannon C Kelly et al.
Redox biology, 27, 101075-101075 (2018-12-24)
The reduction of extracellular oxidants by intracellular electrons is known as trans-plasma membrane electron transport (tPMET). The goal of this study was to characterize a role of tPMET in the sensing of glucose as a physiological signal. tPMET from C2C12
Young J Yauger et al.
Journal of neuroinflammation, 16(1), 41-41 (2019-02-20)
Excessive iron contributes to oxidative stress after central nervous system injury. NADPH oxidase (NOX) enzymes are upregulated in microglia after pro-inflammatory activation and contribute to oxidative stress. The relationship between iron, microglia, NOX, and oxidative stress is currently unclear. We
Mavis A A Tenkorang et al.
Endocrinology, 160(4), 947-963 (2019-02-28)
Oxidative stress (OS) is a common characteristic of several neurodegenerative disorders, including Parkinson disease (PD). PD is more prevalent in men than in women, indicating the possible involvement of androgens. Androgens can have either neuroprotective or neurodamaging effects, depending on
Kazufumi Hirano et al.
Antioxidants & redox signaling, 23(5), 358-374 (2015-07-03)
The NADPH oxidase (NOX) family of enzymes catalyzes the formation of reactive oxygen species (ROS). NOX enzymes not only have a key role in a variety of physiological processes but also contribute to oxidative stress in certain disease states. To
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