LRH-1 ANTAGONIST 1PC X 25MG (C005B-228711)

General description

A cell-permeable pyrazolylbiphenylethanone compound that targets LRH-1/NR5A2 ligand binding domain (LBD) via direct affinity interaction (K_d = 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).

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 using HEK293 transfectants), while exhibiting no inhibitory effect against AR, ERα, or TRβ transcription activity at concentrations up to 10 µM. Reported to exhibits non-cytotoxic antiproliferation activity in LRH-1-expressing cancer cultures (15 to 20 µM), but not pancreatic cancer L3.3 line that does not express LRH-1 (20% inhibition at 40 µM).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
LRH-1

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Benod, C., et al. 2013. J. Biol. Chem.288, 19830.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 375.46. Empirical Formula: C₂₃H₂₅N₃O₂. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: pale yellow. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.