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.

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.

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

VAS2870 is a selective inhibitor of the NADPH oxidases.

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.

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.

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.

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

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.

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.

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.

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

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).

NCATS-SM7270 is a specific small molecule NADPH oxidase 2 (NOX2) inhibitor with IC50 of 2.1 uM (Polymorphonuclear leukocytes, PMN), inhibits NOX2 in primary human and mouse granulocytes.

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.