MHY553

MHY553 is an agonist of peroxisome proliferator-activated receptor α (PPARα).¹ It activates PPARα in HepG2 cells in a reporter assay when used at a concentration of 1 µM but does not activate PPARβ or PPARγ at 10 µM. MHY553 (3 µM) prevents triglyceride accumulation induced by the liver X receptor (LXR) agonist T0901317 in HepG2 cells, as well as scavenges reactive oxygen species (ROS) and peroxynitrite in cell-free assays (IC₅₀s = 39.7 and 2.39 µM, respectively).^1,2 It also inhibits β-glucuronidase and tyrosinase (IC₅₀s = 8.9 and 0.01 µM for the bovine liver and mushroom enzymes, respectively).^3,4 MHY553 (5 mg/kg) reduces age-induced increases in liver weight and triglyceride levels in a rat model of hepatic steatosis.¹

1.Kim, S.M., Lee, B., An, H.J., et al.Novel PPARα agonist MHY553 alleviates hepatic steatosis by increasing fatty acid oxidation and decreasing inflammation during agingOncotarget8(28)46273-46285(2017) 2.Jung, H.J., Kim, S.M., Kim, D.H., et al.2,4-Dihydroxyphenyl-benzo[d]thiazole (MHY553), a synthetic PPARα agonist, decreases age-associated inflammatory responses through PPARα activation and RS scavenging in the skinExp. Gerontol.143111153(2021) 3.Khan, K.M., Rahim, F., Halim, S.A., et al.Synthesis of novel inhibitors of β-glucuronidase based on benzothiazole skeleton and study of their binding affinity by molecular dockingBioorg. Med. Chem.19(14)4286-4294(2011) 4.Ha, Y.M., Park, J.Y., Park, Y.J., et al.Synthesis and biological activity of hydroxy substituted phenyl-benzo[d]thiazole analogues for antityrosinase activity in B16 cellsBioorg. Med. Chem. Lett.21(8)2445-2449(2011)