NCATS-SM7270 is a highly specific small molecule inhibitor of NADPH oxidase 2 (NOX2), exhibiting an IC50 value of 2.1 µM in polymorphonuclear leukocytes (PMN). It effectively inhibits NOX2 activity in both primary human and mouse granulocytes, demonstrating its targeted and potent mechanism of action.

GKT136901 is a potent, selective and orally 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.

TIPTP is a highly potent and selective inhibitor of p22phox, inhibits the p22phox-Rubicon interaction with IC50 of 0.1 uM, and suppresses ROS-mediated inflammation.

LMH001 is a small chemical compound blocking phosphorylated p47phox interaction with p22phox, inhibits effectively angiotensin II (AngII)-induced endothelial Nox2 activation and superoxide production (IC50=0.25 uM).

GLX481304 is a specific small molecule inhibitor of Nox2 and Nox4 with IC50 values of 1.25 uM, shows negligible effects on Nox1.

GLX7013114 (GLX-7013114) is a novel selective NADPH oxidase 4 (Nox4) inhibitor with IC50 of 0.3 uM in in CJ Nox4 HEK 293 cell asays.GLX7013114 displays no activity against Nox 1/2/3/5, as well as Glucose oxidase and Xanthine oxidase; does not display any redox activity.GLX7013114 inhibits TGFβ-induced upregulation of mesenchymal genes.GLX7013114 protected islet cells against both cytokines and high glucose + palmitate.

VAS2870 is a selective inhibitor of the NADPH oxidases.

GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

NOS31 is a potent, selective NADPH oxidase 1 (Nox1) inhibitor with IC50 of 2.0 uM.NOS31 inhibited ROS production in CaCO2 cells in a dose-dependent manner, inhibits NOXO1/NOXA1-induced ROS production.NOS31 is much less potent with other Nox enzymes Nox2, Nox3, Nox4, and Nox5 in HEK293 reconstitution systems (>15-fold selectivity).NOS31 inhibited the proliferation of several colon cancer cell lines in vitro (CaCO2, HT-29, DLD-1, RKO, and HCT-116), with no direct antioxidant activity nor cytotoxity.

gp91ds-tat, a peptide inhibitor for NADPH oxidase assembly, is composed of gp91phox sequence linked to the human immunodeficiency virus-tat peptide. The tat sequence facilitates the entry of this peptide into cells.

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.

GLX351322 is an inhibitor of NADPH oxidase 4, and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μ M.

Mulberrofuran G protects ischemic injury-induced cell death via inhibition of NOX4-mediated ROS generation and ER stress. Mulberrofuran G shows moderate inhibiting activity of hepatitis B virus (HBV) DNA replication with the

NoxA1ds TFA is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds TFA inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.

Fulvene-5 is a potent NADPH oxidase 4 (NOX4) inhibitor with antioxidant properties. Fulvene-5 is a reactive oxygen species (ROS) modifying agent and a potent radioprotector. Fulvene-5 has antitumor activity.