A cell-permeable pyrazolylbiphenylethanone compound that targets LRH-1/NR5A2 ligand binding domain (LBD) via direct affinity interaction (Kd = 1.5 µM), preventing LRH-1 from assuming an active conformation. Shown to antagonize LRH-1-, but not SF-1-, dependent G0S2 transcription (IC50 = 5 µM vs. no inhibition at 10 µM, respectively; 24 h drug treatment commences 3 h after tetracycline induction in HEK293 transfectants), while exhibiting no inhibitory effect against AR (androgen hormone receptor), ERα (estrogen hormone receptor α), or TRβ (thyroid hormone receptor β) transcription activity in HeLa-based reporter transactivation assays at concentrations up to 10 µM. Reported to exhibit non-cytotoxic antiproliferation activity in LRH-1-expressing cancer cultures (Cell line/GI50 = AsPC-1/20 µM, HT-29/15 µM, MDA-MB-468/20 µM, T47D/20 µM), while being much less effective against the proliferation of pancreatic cancer L3.3 line that does not express LRH-1 (20% inhibition at 40 µM).
생화학적/생리학적 작용
Cell permeable: yes
Primary Target LRH-1
Reversible: yes
포장
Packaged under inert gas
경고
Toxicity: Standard Handling (A)
재구성
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
기타 정보
Benod, C., et al. 2013. J. Biol. Chem.288, 19830.
법적 정보
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
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