NADPH Oxidase (NOX)|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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NADPH oxidase (NOX) is a transmembrane enzyme that is located in intracellular organelles. NADPH oxidase (NOX) enzymes are membrane-bound proteins that catalyze the conversion of oxygen to superoxide. There are a number of isoforms, NOX1-5 and dual oxidases 1 and 2 (DUOX1-2), which have diverse functions. NOX1, NOX2, NOX4, and NOX5 are expressed in human vascular tissue. NOX1 and NOX2 are regulated by cytosolic components loosely termed as activators or organizers, which are generally recruited to the membrane components following cellular stimuli to assemble an active NOX. Molecular switch from NOX1 to NOX2 in colon cancer cells induces ROS production and subsequently enhances MMP-7 expression by deactivating AMPK. Vascular NOX4 is a multifarious NADPH oxidase. NOX4 is a hydrogen peroxide-generating oxygen sensor.

Cat. No.	Product Name	CAS No.	Information
H5304	GSK-2795039	1415925-18-6	GSK-2795039 (GSK2795039) is a potent and selective inhibitor of NOX2 (NADPH oxidase 2) with pIC50 of 6.57; exhibits good selectivity for NOX2 over other NOX isoforms, xanthine oxidase and eNOS; abolishes the production of ROS by activated NOX2 enzyme in a paw inflammation model of acute pancreatitis.
H5303	GLX351322	835598-94-2	GLX351322 (GLX-351322) is a novel potent inhibitor of NADPH oxidase 4 (Nox4), inhibits hydrogen peroxide production from tetracycline inducible NOX4-overexpressing cells with IC50 of 5 uM; dispplays an order of magnitude less activity against NOX2; counteracts non-fasting hyperglycemia and impairs glucose tolerance in HFD-treated male C57BL/6 mice, prevents high-glucose-induced human islet cell reactive oxygen species (ROS) production and death.
H5302	GKT137831	1218942-37-0	GKT137831 (Setanaxib, GKT-137831) is a potent, selective, dual NADPH oxidase Nox1/4 inhibitor with Ki of 110/140 nM, 15-fold less potent on Nox2 and 3-fold less potent on Nox5, and no affinity for xanthine oxidase; attenuates liver fibrosis and ROS production in both SOD1mu and WT mice, suppresses ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT in hepatic stellate cells (HSCs).
H5301	APX-115 freebase	1270084-92-8	APX-115 (Isuzinaxib,Ewha 18278) is a first-in-class, orally active, pan-NADPH oxidase (Nox) inhibitor with Ki of 1.08, 0.57, 0.63 nM for Nox1, Nox2, and Nox4, respectively; shows no inhibitory activities on xanthine oxidase and glucose oxidase; inhibits the responses of BMMs to RANKL, including ROS generation, activation of MAPK and NF-κB, and osteoclast cells differentiation; protects db/db mice from renal injury.
H5300	APX-115	1395946-75-4	APX-115 (Ewha 18278) is a first-in-class, orally active, pan-NADPH oxidase (Nox) inhibitor with Ki of 1.08, 0.57, 0.63 nM for Nox1, Nox2, and Nox4, respectively; shows no inhibitory activities on xanthine oxidase and glucose oxidase; inhibits the responses of BMMs to RANKL, including ROS generation, activation of MAPK and NF-κB, and osteoclast cells differentiation; protects db/db mice from renal injury.
H5308	VAS-2870	722456-31-7	A potent, specific NADPH oxidase (Nox) inhibitor; completely abolishes PDGF-mediated NAD(P)H oxidase activation and ROS production at 10-20 uM in vascular smooth muscle cells (VSMC); abrogates thalidomide stimulation of cardiomyogenesis; also impairs cell growth and enhances TGF-β-induced apoptosis of liver tumor cells.
H5307	ML090	531-46-4	ML090 (ML-090, CCG-44699, Fluoflavin, NSC 179821) is a potent, selecitve inhibitor of NADPH oxidase 1 (NOX1) with IC50 of 90 nM, displays no significant activities against NOX2, 3 and 4 (IC50>10 uM).
H5306	ML 171	6631-94-3	A potent, specific, cell-active NADPH oxidase1 (Nox1) inhibitor that strongly blocks ROS generation in HT29 cells with IC50 of 0.129 uM; shows only marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms; also blocks the ROS-dependent formation of ECM-degrading invadopodia in colon cancer cells.
H5305	Imipramine Blue	1169943-24-1	A potent STAT5 inhibitor with a dual mechanism of action, potently inhibits STAT5 through liberation of endogenous phosphatase activity following NADPH oxidase (NOX) inhibition at 200-300 nM; effectively kills mutant FLT3-driven AML cells through a similar mechanism as thapsigargin (TG), involving increased cytosolic calcium, at 75-150 nM; a novel anti-invasive small molecule that inhibits invasion of glioma in vitro.
H8380	GKT136901	955272-06-7	GKT136901 is a potent, selective and oral active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 also is a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.

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