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538339 HuR-ARE Interaction Inhibitor, CMLD-2 - Calbiochem

A cell-permeable compound that competitively binds to Hu antigen R (HuR; Ki = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs.

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Synonyme: 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one

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538339
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      Description
      OverviewA cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR; Ki = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs. Displays dose-dependent binding to full-length HuR protein and to RRM1/2 fragment. Exhibits cytotoxicity towards tumor cells and reduces their viability (IC50 = 28.9 and 18.2 µM for HCT-116 and MioPaCa2 cells, respectively). Has much reduced effect on normal WI-38 and CCD 841 CoN cells. Shown to induce cleavage of poly (ADP-ribose) polymerase and pro-caspase 3 (~ 50 µM) and reduce the half-life of Bcl-2, Msi1, and XIAP in HCT-116 cells (~20 µM) treated with actinomycin D (5 µg/ml).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number538339
      Brand Family Calbiochem®
      Synonyms5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one
      DescriptionHuR-ARE Interaction Inhibitor, CMLD-2
      References
      ReferencesWu, X., et al. 2015. ACS Chem. Biol. 10, 1476.
      Product Information
      FormWhite solid
      Hill FormulaC₃₁H₃₁NO₆
      Chemical formulaC₃₁H₃₁NO₆
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetHuR
      Primary Target K<sub>i</sub>350 nM for HuR binding
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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°:). Stock solutions are stable for up to months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      5383390001 04054839119576

      Documentation

      HuR-ARE Interaction Inhibitor, CMLD-2 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Wu, X., et al. 2015. ACS Chem. Biol. 10, 1476.
      Datenblatt

      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.

      Revision23-September-2016 JSW
      Synonyms5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one
      DescriptionA cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR; Ki = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs. Displays dose-dependent binding to full-length HuR protein and to RRM1/2 fragment. Exhibits cytotoxicity towards tumor cells and reduces their viability (IC50 = 28.9 and 18.2 µM for HCT-116 and MioPaCa2 cells, respectively). Has much reduced effect on normal WI-38 and CCD 841 CoN cells. Shown to induce cleavage of poly (ADP-ribose) polymerase and pro-caspase 3 (~ 50 µM) and reduce the half-life of Bcl-2, Msi1, and XIAP in HCT-116 cells (~20 µM) treated with actinomycin D (5 µg/ml).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₁H₃₁NO₆
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°:). Stock solutions are stable for up to months at -20°C.
      Toxicity Standard Handling
      ReferencesWu, X., et al. 2015. ACS Chem. Biol. 10, 1476.