532718 BRPF1 BD Inhibitor - Calbiochem

532718
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₂₆N₄O₃

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable dimethyl-benzimidazolone compound that acts as a highly potent, reversible, and acetylated lysine-competitive inhibitor of BRPF1 bromodomain (IC50 = 80 nM; Kd = 10 nM). Acts by displacing BRPF1 bromodomain from histone H3.3 (IC50 = 0.98 µM). Shown to directly interact with BRPF1 BD and display excellent selectivity over other bromodomains, such as BET (bromodomain and extra terminal), BRPF2 (pIC50 = 5.1), BRPF3 (pIC50 ≤ 4.0), and BRD4 B1 and BD2 (pIC50 ≤ 4.3).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532718
      Brand Family Calbiochem®
      SynonymsN-(1,3-Dimethyl-2-oxo-6-(1-piperidinyl)-2,3-dihydro-1H-benzimidazol-5-yl)-2-methoxybenzamide, Bromodomain and PHD Finger-containing 1 BD Inhibitor, BRPF1 Bromodomain Inhibitor
      References
      ReferencesDemont, E.H., et al. 2014. ACS Med. Chem. Lett. 5, 1190.
      Product Information
      FormWhite solid
      Hill FormulaC₂₂H₂₆N₄O₃
      Chemical formulaC₂₂H₂₆N₄O₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetBRPF1 BD
      Primary Target K<sub>i</sub>10 nM)
      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

      BRPF1 BD Inhibitor - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Demont, E.H., et al. 2014. ACS Med. Chem. Lett. 5, 1190.
      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.

      Revision18-March-2015 JSW
      SynonymsN-(1,3-Dimethyl-2-oxo-6-(1-piperidinyl)-2,3-dihydro-1H-benzimidazol-5-yl)-2-methoxybenzamide, Bromodomain and PHD Finger-containing 1 BD Inhibitor, BRPF1 Bromodomain Inhibitor
      DescriptionA cell-permeable dimethyl-benzimidazolone compound that exhibits BRPF1-selective bromodomain (BD) affinity (Kd = 10 nM) by targeting the acetyl-lysine (KAc) pocket, while exhibiting much reduced or little affinity toward BDs from 34 other proteins, including bromodomain and PHD finger-containing (BRPF) family members BRPF2 (BRD1) and BRPF3 (Kd = 879 nM and 3.1 µM, respectively). BRPF1 selectivity is also demonstrated by FRET-based competitive binding studies (pIC50 against ligand binding = 7.3 to 4.7/BRPF1, ≤ 5.6/BRPF2, ≤ 4.8/BRPF3, ≤ 5.8/BRD4 BD1, ≤ 5.0/BRD4 BD2; [Ligand] used = Kd of respective ligand). Shown to selectively prevent histone H3.3 interaction with BRPF1 BD in HEK293 cells (IC50 = 0.98 µM), while displaying little potency against histone H3.3 interaction with BRPF1 BD isoform 2 that contains a 6-amino acid insert close to the KAc-binding site.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₂₆N₄O₃
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml). Use only fresh DMSO for reconstitution.
      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
      ReferencesDemont, E.H., et al. 2014. ACS Med. Chem. Lett. 5, 1190.