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505760 HDAC6 Inhibitor II, BRD9757 - CAS 1423058-85-9 - Calbiochem

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Synonymes: HDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI, N-Hydroxycyclopent-1-enecarboxamide

Primary Target: HDAC6
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505760
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Tableau de caractéristiques principal

CAS #Empirical Formula
1423058-85-8C₆H₉NO₂

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      Description
      OverviewA cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced potency against class IIa HDAC4/5/7/9 (IC50 >12.61 µM). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation in HeLa cells (10 & 30 µM; 24 h) without inducing histone H3 acetylation increase seen with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187). Unlike other Zinc-binding group-containing HDAC inhibitors, BRD9757 does not contain an apparent selectivity-imparting capping structure linked to its hydroxamate.
      Catalogue Number505760
      Brand Family Calbiochem®
      SynonymsHDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI, N-Hydroxycyclopent-1-enecarboxamide
      References
      ReferencesWagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.
      Product Information
      CAS number1423058-85-8
      FormPale orange solid
      Hill FormulaC₆H₉NO₂
      Chemical formulaC₆H₉NO₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetHDAC6
      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 6 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
      5057600001 04055977243505

      Documentation

      HDAC6 Inhibitor II, BRD9757 - CAS 1423058-85-9 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Wagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.

      Informations techniques

      Titre
      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
      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.

      Revision03-September-2020 JSW
      SynonymsHDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI, N-Hydroxycyclopent-1-enecarboxamide
      DescriptionA cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced or little potency against class IIa HDAC4/5/7/9 (IC50 = 21.80, 18.32, 12.61, and >33.33 µM, respectively). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation level in HeLa cells (10 & 30 µM; 24 h) without inducing detectable histone H3 acetylation increase seen in cells treated with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187) or the general HDAC inhibitor SAHA. BRD9757 does not contain an apparent selectivity-imparting capping structure linked to the zinc-binding hydroxamate as seen in other ZBG- (Zinc binding group) containing HDAC inhibitors.
      FormPale orange solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1423058-85-8
      Chemical formulaC₆H₉NO₂
      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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesWagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.