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534354 p300/CBP Inhibitor X, EML425

A cell-permeable, potent, reversible, non-competitive, and selective inhibitor of p300/CBP (IC₅₀ = 2.9 µM and 1.1 µM, respectively).

p300/CBP Inhibitor X, EML425 : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione, EML-425, p300/CBP Acetyltransferase Inhibitor, EML425

Primary Target: p300/CBP
534354
Purchase on Sigma-Aldrich

Aperçu

Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₂₇H₂₄N₂O₄

Products

RéférenceConditionnement Qté
5343540001 Flacon en verre 10 mg
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
Quality LevelMQ100
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
Global Trade Item Number
Référence GTIN
5343540001 04054839117268

Documentation

p300/CBP Inhibitor X, EML425 FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Milite, C., et al. 2015. J. Med. Chem. 58, in press.
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.

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 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 3 months at -20°C.
Toxicity Standard Handling
ReferencesMilite, C., et al. 2015. J. Med. Chem. 58, in press.