5.05601

LRH-1 Antagonist

• 동의어(들): LRH-1 Antagonist, Liver Receptor Homologue 1 Antagonist, NR5A2 Antagonist, Nuclear Receptor Subfamily 5 Group A Member 2 Antagonist, 1-(3ʹ-(1-(2-Morpholinoethyl)-1H-pyrazol-3-yl)biphenyl-3-yl)ethanone, 1-(3ʹ-(1-(2-(4-Morpholinyl)ethyl)-1H-pyrazol-3-yl)-3-biphenylyl)ethanone, Nuclear Receptor Subfamily 5 Group A Member 2 Antagonist, 1-(3ʹ-(1-(2-Morpholinoethyl)-1H-pyrazol-3-yl)biphenyl-3-yl)ethanone, 1-(3ʹ-(1-(2-(4-Morpholinyl)ethyl)-1H-pyrazol-3-yl)-3-biphenylyl)ethanone, Liver Receptor Homologue 1 Antagonist, NR5A2
• 실험식(Hill 표기법): C₂₃H₂₅N₃O₂
• CAS Number: 1185410-60-9
• Molecular Weight: 375.46
• MDL number: MFCD00010900
• UNSPSC 코드: 41106200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: pale yellow
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

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).

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable