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 (Item No. 71810) 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

WARNING This product is not for human or veterinary use.

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 aging. Oncotarget 8(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 skin. Exp. Gerontol. 143, 111153 (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 docking. Bioorg. 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 cells. Bioorg. Med. Chem. Lett. 21(8), 2445-2449 (2011).