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Description

A cell-permeable pyrazolylbiphenylethanone compound that targets LRH-1/NR5A2 ligand binding domain (LBD) via direct affinity interaction (Kd = 1.5 µ,M), preventing LRH-1 from assuming an active conformation. Shown to antagonize LRH-1-, but not SF-1-, dependent G0S2 transcription (IC50 = 5 µ,M vs. no inhibition at 10 µ,M, respectively, 24 h drug treatment commences 3 h after tetracycline induction in HEK293 transfectants), while exhibiting no inhibitory effect against AR (androgen hormone receptor), ERalpha (estrogen hormone receptor alpha), or TRbeta (thyroid hormone receptor beta) transcription activity in HeLa-based reporter transactivation assays at concentrations up to 10 µ,M. Reported to exhibit non-cytotoxic antiproliferation activity in LRH-1-expressing cancer cultures (Cell line/GI50 = AsPC-1/20 µ,M, HT-29/15 µ,M, MDA-MB-468/20 µ,M, T47D/20 µ,M), while being much less effective against the proliferation of pancreatic cancer L3.3 line that does not express LRH-1 (20% inhibition at 40 µ,M)., A cell-permeable pyrazolylbiphenylethanone compound that targets LRH-1/NR5A2 ligand binding domain (LBD) via direct affinity interaction (Kd = 1.5 µ,M), preventing LRH-1 from assuming an active conformation. Shown to antagonize LRH-1-, but not SF-1-, dependent G0S2 transcription (IC50 = 5 µ,M using HEK293 transfectants), while exhibiting no inhibitory effect against AR, ERalpha, or TRbeta transcription activity at concentrations up to 10 µ,M. Reported to exhibits non-cytotoxic antiproliferation activity in LRH-1-expressing cancer cultures (15 to 20 µ,M), but not pancreatic cancer L3.3 line that does not express LRH-1 (20% inhibition at 40 µ,M).