BH400 is an agonist of peroxisome proliferator-activated receptor α (PPARα) and an inhibitor of stimulator of interferon genes (STING; IC50 = 8.1 ?M).1 It induces transactivation of PPARα in a reporter assay using THP-1 cells (EC50 = 1.2 ?M). BH400 (10 ?M) inhibits decreases in viability induced by 4-hydroxy nonenal (4-HNE or hydrogen peroxide (H2O2) in 661W retinal ganglion cells. It prevents LPS-induced increases in phosphorylated TANK-binding kinase 1 (TBK1) and IL-6 levels and LPS-induced decreases in peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) levels in HMC3 microglial cells when used at a concentration of 10 ?M.
References:
[1]. Hu, B., Cui, Y., Lee, J.J., et al.Design and assessment of first-generation heterobifunctional PPARα/STING modulatorsACS Med. Chem. Lett.15(8)1279-1286(2024).