GSK2795039

Catalog No.S8974

For research use only.

GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.

GSK2795039 Chemical Structure

CAS No. 1415925-18-6

Purity & Quality Control

Choose Selective NADPH-oxidase Inhibitors

Biological Activity

Description GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.
Targets
ROS [2]
()
NADPH [2]
()
NOX2 (HRP/Amplex Red) [1]
(Cell-based assay)
6.57(pIC50)
In vitro

GSK2795039 inhibits both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. GSK2795039 inhibits NOX2 in an NADPH competitive manner and is selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes.[1]

In vivo

Following systemic administration in mice, GSK2795039 abolishes the production of ROS by activated NOX2 enzyme in a paw inflammation model. GSK2795039 shows activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: NOX isoform-specific cells, PBMCs, PMNs, HL60 cells
  • Concentrations: 3.16 nM, 10 nM, 31.6 nM, 100 nM, 316 nM, 1μM, 3.16 μM, 10 μM, 31.6 μM, 100μM
  • Incubation Time: 10 min, 20 min, 30 min, 40 min, 50 min, 60 min
  • Method:

    For Amplex Red/HRP assay, cells are preincubated with the GSK2795039 for 10 min at room temperature in PerkinElmer black 96-well microplates at 50,000 cells per well, after which the reaction mixture is added to a final concentration of 25 μM of Amplex Red and 0.05 U/ml of HRP in HBSS. NOX enzymes are activated via 100 nM PMA (NOX1, NOX2), 1 μg/ml tetracycline for 24-h activation of inducible genes (NOX3, NOX4), and 1 μM Ca2+ ionophore ionomycin (NOX5).

Animal Research:

[1]

  • Animal Models: Male Sprague-Dawley (SD) rats, C57BL6/J mice, gp91phox knockout mice
  • Dosages: 2–100 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

DMSO 90 mg/mL
(199.75 mM)
Ethanol 20 mg/mL
(44.38 mM)
Water Insoluble

Chemical Information

Molecular Weight 450.56
Formula

C23H26N6O2S

CAS No. 1415925-18-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N1C=C(C2=C(C=CN=C21)NS(=O)(=O)C3=NN(C=C3)C)C4=CC5=C(CCN5C)C=C4

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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