GK-136901 

GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a K_i of 160 nM for Nox1 and 165 nM for Nox4. GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin (fibronectin) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension^[1][2][3][4].

GKT136901 (10 μM; 30 min) inhibits NADPH oxidase activity and ROS production induced by high D-glucose in MPT cells^[2].
GKT136901 (10 μM; 30 min) inhibits the expression of profibrotic proteins and the activation of p38MAP kinase in MPT cells induced by high D-glucose^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GK-136901 attenuates hypoxia-induced pulmonary vascular cell proliferation in a mouse model of pulmonary arterial hypertension^[4].
GK-136901 is well tolerated in mice, with oral administration doses tested up to 1000 mg/kg^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

346.38

C₂₀H₁₈N₄O₂

1062624-71-8

O=C1C=C2NN(C3=C(C)C=CC=C3)C(C2=C(C)N1CC4=NC=CC=C4)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Weaver J R, Grzesik W, Taylor-Fishwick D A. Inhibition of NADPH oxidase-1 preserves beta cell function[J]. Diabetologia, 2015, 58(1): 113-121.

  [2]. Harrison IP, et al. Understanding the biology of reactive oxygen species and their link to cancer: NADPH oxidases as novel pharmacological targets. Clin Exp Pharmacol Physiol. 2014;41(8):533-542.  [Content Brief]

  [3]. Sedeek M, et al. Critical role of Nox4-based NADPH oxidase in glucose-induced oxidative stress in the kidney: implications in type 2 diabetic nephropathy[J]. American Journal of Physiology-Renal Physiology, 2010, 299(6): F1348-F1358.

  [4]. Schramm A, et al. Targeting NADPH oxidases in vascular pharmacology. Vascul Pharmacol. 2012;56(5-6):216-231.  [Content Brief]

  [5]. Rodiño-Janeiro BK, et al. Current status of NADPH oxidase research in cardiovascular pharmacology. Vasc Health Risk Manag. 2013;9:401-428.  [Content Brief]