SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ).1 It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid to PPARγ in a time-resolved FRET (TR-FRET) assay.
References
1. Brust, R., Lin, H., Fuhrmann, J., et al. Modification of the orthosteric PPARγ covalent antagonist scaffold yields an improved dual-site allosteric inhibitor. ACS Chem. Biol. 12(4), 969-978 (2017).
















