5.34354

p300/CBP Inhibitor X, EML425

• Sinônimo(s): p300/CBP Inhibitor X, EML425, 1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione, EML-425, p300/CBP Acetyltransferase Inhibitor, EML425
• Fórmula empírica (Notação de Hill): C₂₇H₂₄N₂O₄
• Peso molecular: 440.49
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

A 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).

A 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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
p300/CBP

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Milite, C., et al. 2015. J. Med. Chem.58, in press.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable