For research use only. Not for therapeutic Use.
GKT-137831（Cat No.:I000837）is a selective inhibitor of NADPH oxidase (NOX) isoforms NOX1 and NOX4, enzymes involved in generating reactive oxygen species (ROS) that contribute to oxidative stress. By targeting NOX1 and NOX4, GKT-137831 helps reduce oxidative damage and inflammation, making it valuable in researching fibrotic, renal, and cardiovascular diseases where NOX-driven ROS play a critical role. Its antioxidant and anti-fibrotic properties have shown promise in preclinical models, particularly in conditions like diabetic nephropathy, pulmonary fibrosis, and liver fibrosis, positioning it as a potential therapeutic in oxidative stress-related disorders.
| Catalog Number | I000837 |
| CAS Number | 1218942-37-0 |
| Synonyms | 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione |
| Molecular Formula | C₂₁H₂₀ClN₄O₂ |
| Purity | ≥95% |
| Target | NADPH Oxidase |
| Solubility | DMSO: ≥ 37 mg/mL |
| Storage | Store at -20°C |
| IC50 | 140±40 nM/110±30 nM(Nox1/Nox4, Ki) |
| IUPAC Name | 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6-dione |
| InChI | InChI=1S/C21H19ClN4O2/c1-24(2)14-8-6-7-13(11-14)20-19-16(12-18(27)25(20)3)23-26(21(19)28)17-10-5-4-9-15(17)22/h4-12,23H,1-3H3 |
| InChIKey | RGYQPQARIQKJKH-UHFFFAOYSA-N |
| SMILES | CN1C(=O)C=C2C(=C1C3=CC(=CC=C3)N(C)C)C(=O)N(N2)C4=CC=CC=C4Cl |
| Reference | </br>1:Combined NOX1/4 inhibition with GKT137831 in mice provides dose-dependent reno- and atheroprotection even in established micro- and macrovascular disease. Gray SP, Jha JC, Kennedy K, van Bommel E, Chew P, Szyndralewiez C, Touyz RM, Schmidt HH, Cooper ME, Jandeleit-Dahm KA.Diabetologia. 2017 May;60(5):927-937. doi: 10.1007/s00125-017-4215-5. Epub 2017 Feb 3. PMID: 28160092 </br>2:Early oxidative damage induced by doxorubicin: Source of production, protection by GKT137831 and effect on Ca(2+) transporters in HL-1 cardiomyocytes. Asensio-López MC, Soler F, Sánchez-Más J, Pascual-Figal D, Fernández-Belda F, Lax A.Arch Biochem Biophys. 2016 Mar 15;594:26-36. doi: 10.1016/j.abb.2016.02.021. Epub 2016 Feb 22. PMID: 26906075 </br>3:The Nox1/4 Dual Inhibitor GKT137831 or Nox4 Knockdown Inhibits Angiotensin-II-Induced Adult Mouse Cardiac Fibroblast Proliferation and Migration. AT1 Physically Associates With Nox4. Somanna NK, Valente AJ, Krenz M, Fay WP, Delafontaine P, Chandrasekar B.J Cell Physiol. 2016 May;231(5):1130-41. doi: 10.1002/jcp.25210. Epub 2015 Oct 19. PMID: 26445208 Free PMC Article</br>4:Inhibition of NOX1/4 with GKT137831: a potential novel treatment to attenuate neuroglial cell inflammation in the retina. Deliyanti D, Wilkinson-Berka JL.J Neuroinflammation. 2015 Jul 30;12:136. doi: 10.1186/s12974-015-0363-z. PMID: 26219952 Free PMC Article</br>5:The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. Green DE, Murphy TC, Kang BY, Kleinhenz JM, Szyndralewiez C, Page P, Sutliff RL, Hart CM.Am J Respir Cell Mol Biol. 2012 Nov;47(5):718-26. doi: 10.1165/rcmb.2011-0418OC. Epub 2012 Aug 16. PMID: 22904198 Free PMC Article</br>6:Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Aoyama T, Paik YH, Watanabe S, Laleu B, Gaggini F, Fioraso-Cartier L, Molango S, Heitz F, Merlot C, Szyndralewiez C, Page P, Brenner DA.Hepatology. 2012 Dec;56(6):2316-27. doi: 10.1002/hep.25938. PMID: 22806357 Free PMC Article</br>7:Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo. Jiang JX, Chen X, Serizawa N, Szyndralewiez C, Page P, Schröder K, Brandes RP, Devaraj S, Török NJ.Free Radic Biol Med. 2012 Jul 15;53(2):289-96. doi: 10.1016/j.freeradbiomed.2012.05.007. Epub 2012 May 19. PMID: 22618020 Free PMC Article |
