EML 425

SKU: orb1308340

Description

EML 425 is a small molecule inhibitor that potently and selectively targets the CBP and p300 bromodomains, with respective IC50 values of 2.9 µM and 1.1 µM. This compound is a valuable chemical probe for epigenetic research, used in vitro to investigate the roles of these transcriptional coactivators in cancer and cellular differentiation pathways.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1675821-32-5
• MW: 440.49
• Purity: >99.99% (May vary between batches)
• Formula: C₂₇H₂₄N₂O₄
• SMILES: Cc1cc(O)cc(C)c1C=C1C(=O)N(Cc2ccccc2)C(=O)N(Cc2ccccc2)C1=O
• Target: Epigenetic Reader Domain,Histone Acetyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.35 mM);DMSO:250 mg/mL (567.55 mM)

Bioactivity

• Target IC50:
  CBP:2.9 μM|p300:1.1 μM
• In Vitro:
  EML 425 is shown to be a reversible inhibitor, noncompetitive versus both acetyl-CoA and a histone H3 peptide, and able to bind both the free enzyme and the enzyme-substrate complex, even with unequal affinity constants. EML 425, noncompetitive versus both acetyl-CoA and a histone H3 peptide, shows good cell permeability. EML 425 inhibits both p300 and CBP (IC50 values of 2.9 and 1.1 μM, respectively) while being practically inactive against the enzymes general control non-derepressible-5 (GCN5) and p300/CBP-associated factor (PCAF). EML 425 causes a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9 in U937 cells. The binding site for EML 425 is an alternative pocket lying near the substrate lysine binding groove and close to the acetylation site.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CBP, p300, inhibit, EML425, EML-425, EML 425, EpigeneticReaderDomain, Epigenetic Reader Domain, Inhibitor, Histone Acetyltransferase, HistoneAcetyltransferase, HATs, HAT

Compound Identifiers

PubChem CID

91826273