505601 | LRH-1 Antagonist - Calbiochem

505601
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₅N₃O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05601.0001
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          Glass bottle 25 mg
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          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, 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
          References
          ReferencesBenod, C., et al. 2013. J. Biol. Chem. 288, 19830.
          Product Information
          FormPale yellow solid
          Hill FormulaC₂₃H₂₅N₃O₂
          Chemical formulaC₂₃H₂₅N₃O₂
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          Documentation

          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, 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
          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
          Chemical formulaC₂₃H₂₅N₃O₂
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesBenod, C., et al. 2013. J. Biol. Chem. 288, 19830.