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

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Synonymes: Nuclear Receptor Subfamily 5 Group A Member 2 Antagonist, Liver 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

Primary Target: LRH-1
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505601
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Tableau de caractéristiques principal

CAS #Empirical Formula
1185410-60-9C₂₃H₂₅N₃O₂

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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®
      SynonymsNuclear Receptor Subfamily 5 Group A Member 2 Antagonist, Liver 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
      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
      Référence GTIN
      5056010001 04055977243390

      Documentation

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

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Benod, C., et al. 2013. J. Biol. Chem. 288, 19830.
      Fiche technique

      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
      SynonymsNuclear Receptor Subfamily 5 Group A Member 2 Antagonist, Liver 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
      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.