A NOX2 inhibitor
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GSK2795039

Item No. 33777

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(2,3-dihydro-1-methyl-1H-indol-6-yl)-1-(1-methylethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-methyl-1H-pyrazole-3-sulfonamide
CAS Number
1415925-18-6
Molecular Formula
C23H26N6O2S
Formula Weight
450.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
234 nm
SMILES
O=S(NC1=CC=NC2=C1C(C3=CC(N(CC4)C)=C4C=C3)=CN2C(C)C)(C5=NN(C)C=C5)=O
InChi Code
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)
InChi Key
FMWVTCZKCXPKFW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

    $160

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    25 mg

    $318

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    Product Description

    GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2; IC50 = 0.269 µM).1 It is selective for NOX2 over NOX1, -3, -4, and -5 (IC50s = >1,000 µM for all), as well as xanthine oxidase and PKCβ (IC50s = 28.8 and 10 µM, respectively). GSK2795039 inhibits NOX2-mediated production of reactive oxygen species (ROS) and NADPH depletion in cell-free assays (IC50s = 0.537 and 0.251 µM, respectively). In vivo, GSK2795039 (100 mg/kg) reduces serum levels of amylase, a marker for pancreatic cell necrosis, in a gp91phox knockout mouse model of acute pancreatitis. GSK2795039 also inhibits brain NOX2 activity, decreases neurite shortening and apoptosis, and attenuates neurological deficits in a mouse model of weight drop-induced traumatic brain injury (TBI).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hirano, K., Chen, W.S., Chueng, A.L.W., et al. Discovery of GSK2795039, a novel small molecule NADPH oxidase 2 inhibitor. Antioxid. Redox Signal. 23(5), (2015).

    2. Wang, M., and Luo, L. An effective NADPH oxidase 2 inhibitor provides neuroprotection and improves functional outcomes in animal model of traumatic brain injury. Neurochem. Res. 45(5), 1097-1106 (2020).