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

505760
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₆H₉NO₂ 1423058-85-9

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      5.05760.0001
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          Glass bottle 10 mg
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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®
          SynonymsN-Hydroxycyclopent-1-enecarboxamide, HDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI
          References
          ReferencesWagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.
          Product Information
          CAS number1423058-85-9
          FormPale orange solid
          Hill FormulaC₆H₉NO₂
          Chemical formulaC₆H₉NO₂
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Wagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.

          Technical Info

          Title
          White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
          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.

          Revision09-December-2013 JSW
          SynonymsN-Hydroxycyclopent-1-enecarboxamide, HDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI
          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 number1423058-85-9
          Chemical formulaC₆H₉NO₂
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesWagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.