534354 p300/CBP Inhibitor X, EML425

534354
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₇H₂₄N₂O₄

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.34354.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable benzylidenbarbituric acid derivative that acts as a potent, selective inhibitor of lysine acetyltransferase p300/CBP paralogues (IC50 = 2.9 µM and 1.1 µM for recombinant p300 and CBP, respectively). The inhibition appears to be reversible and is non-competitive with respect to both acetyl-CoA and a histone H3 peptide. It binds to both the free enzyme and the enzyme-substrate complex with uneven affinities. Does not affect the activity of general control non-derepressible 5 (GCN5) and p300/CBP-associated factor (PCAF). Shown to reduce the acetylation of lysine H4K5 and H3K9 in U937 cells (~100 µM) and induce a cell cycle arrest at the G0/G1 phase with an increase in the percentage of hypodiploid nuclei (~ 100 µM).

          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 Number534354
          Brand Family Calbiochem®
          Synonyms1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione, EML-425, p300/CBP Acetyltransferase Inhibitor, EML425
          Descriptionp300/CBP Inhibitor X, EML425
          References
          ReferencesMilite, C., et al. 2015. J. Med. Chem. 58, in press.
          Product Information
          FormYellow solid
          Hill FormulaC₂₇H₂₄N₂O₄
          Chemical formulaC₂₇H₂₄N₂O₄
          ReversibleY
          Applications
          Biological Information
          Primary Targetp300/CBP
          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°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

          p300/CBP Inhibitor X, EML425 SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Milite, C., et al. 2015. J. Med. Chem. 58, in press.
          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-September-2016 JSw
          Synonyms1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione, EML-425, p300/CBP Acetyltransferase Inhibitor, EML425
          DescriptionA cell-permeable benzylidenbarbituric acid derivative that acts as a potent, selective inhibitor of lysine acetyltransferase p300/CBP paralogues (IC50 = 2.9 µM and 1.1 µM for recombinant p300 and CBP, respectively). The inhibition appears to be reversible and is non-competitive with respect to both acetyl-CoA and a histone H3 peptide. It binds to both the free enzyme and the enzyme-substrate complex with uneven affinities. Does not affect the activity of general control non-derepressible 5 (GCN5) and p300/CBP-associated factor (PCAF). Shown to reduce the acetylation of lysine H4K5 and H3K9 in U937 cells (~100 µM) and induce a cell cycle arrest at the G0/G1 phase with an increase in the percentage of hypodiploid nuclei (~ 100 µM).
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₇H₂₄N₂O₄
          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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesMilite, C., et al. 2015. J. Med. Chem. 58, in press.