PTGR2-IN-1

349093-44-3

310.39

10 mM in DMSO

Others

PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC₅₀ of ca.0.7 uM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARgamma transcriptional activity in PTGR2-transfected HEK293T cells^[1]. In Vitro: A screen of structural analogs of 20 identified PTGR2-IN-1, which shows substantially increased potency (>20-fold) in assays measuring either competition of 8-labeling or 15-keto-PGE2 reductase activity (IC50 = 0.6 uM) of recombinant PTGR2, as well as an inactive control compound 23. PTGR2-IN-1 (Compound 22) blocks FFF 8 labeling of endogenous PTGR2 in HEK293T cells with good potency (complete inhibition at 5 uM and ca.80% inhibition at 500 nM) and excellent selectivity^[1].