532718 BRPF1 BD Inhibitor - Calbiochem

532718
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₆N₄O₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.32718.0001
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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
          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.