GKT136901

GKT136901 is a dual inhibitor of NADPH oxidase 1 (NOX1) and NOX4 (Kis = 160 and 165 nM, respectively). It is selective for NOX1 and NOX4 over NOX2 and xanthine oxidase (Kis = 1,530 and >30,000 nM, respectively), as well as over a panel of 18 enzymes and ion channels at 10 µM. GKT136901 (0.1, 1, and 10 µM) scavenges peroxynitrite radicals, as well as prevents the nitration and dimerization of alpha-synuclein, in cell-free assays. It prevents peroxynitrite-induced cell death of differentiated LUHMES cells when used at a concentration of 10 µM.Formal Name: 2-(2-chlorophenyl)-4-methyl-5-(2-pyridinylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione. CAS Number: 955272-06-7. Synonyms: NOX Inhibitor IV. Molecular Formula: C19H15ClN4O2. Formula Weight: 366.8. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml, Ethanol: 1 mg/ml. lambdamax: 214, 257 nm. SMILES: O=C1C=C2NN(C3=C(Cl)C=CC=C3)C(C2=C(C)N1CC4=CC=CC=N4)=O. InChi Code: InChI=1S/C19H15ClN4O2/c1-12-18-15(10-17(25)23(12)11-13-6-4-5-9-21-13)22-24(19(18)26)16-8-3-2-7-14(16)20/h2-10,22H,11H2,1H3. InChi Key: DNKYHHFCPXKFIY-UHFFFAOYSA-N.