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505601 LRH-1 Antagonist - CAS 1185410-60-9 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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

Primary Target: LRH-1
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1185410-60-9C₂₃H₂₅N₃O₂

Products

Catalogue NumberPackaging Qty/Pack
5.05601.0001 Glass bottle 25 mg
Description
OverviewA 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).
Catalogue Number505601
Brand Family Calbiochem®
SynonymsLiver 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
References
ReferencesBenod, C., et al. 2013. J. Biol. Chem. 288, 19830.
Product Information
CAS number1185410-60-9
FormPale yellow solid
Hill FormulaC₂₃H₂₅N₃O₂
Chemical formulaC₂₃H₂₅N₃O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetLRH-1
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.05601.0001 04055977243390

Documentation

LRH-1 Antagonist - CAS 1185410-60-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Benod, C., et al. 2013. J. Biol. Chem. 288, 19830.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision22-November-2013 JSW
SynonymsLiver 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
DescriptionA 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).
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1185410-60-9
Chemical formulaC₂₃H₂₅N₃O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesBenod, C., et al. 2013. J. Biol. Chem. 288, 19830.