GSK2795039

GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 reduces apoptosis.

Product information

CAS Number: 1415925-18-6

Molecular Weight: 450.56

Formula: C23H26N6O2S

Chemical Name: 1-methyl-N-[3-(1-methyl-2, 3-dihydro-1H-indol-6-yl)-1-(propan-2-yl)-1H-pyrrolo[2, 3-b]pyridin-4-yl]-1H-pyrazole-3-sulfonamide

Smiles: CN1CCC2=CC=C(C=C12)C1=CN(C(C)C)C2=NC=CC(NS(=O)(=O)C3C=CN(C)N=3)=C12

InChiKey: FMWVTCZKCXPKFW-UHFFFAOYSA-N

InChi: InChI=1S/C23H26N6O2S/c1-15(2)29-14-18(17-6-5-16-8-11-27(3)20(16)13-17)22-19(7-10-24-23(22)29)26-32(30,31)21-9-12-28(4)25-21/h5-7,9-10,12-15H,8,11H2,1-4H3,(H,24,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 32 mg/mL (71.02 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GSK2795039 (25 μM; 24 hours) reduces the combinatory effect of FeSO4 and LPS-increased levels of apoptosis and reduced the presence of caspase-3-positive PC12 cells.

In Vivo:

GSK2795039 (intraperitoneal injection; 100 mg/kg; 1 hour before) decreases activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein.

References:

1. Hirano K, et al. Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor. Antioxid Redox Signal. 2015 Aug 10;23(5):358-74.
2. Yauger YJ, et al. Iron accentuated reactive oxygen species release by NADPH oxidase in activated microglia contributes to oxidative stress in vitro. J Neuroinflammation. 2019 Feb 18;16(1):41.

Products are for research use only. Not for human use.