1. Epigenetics
  2. Histone Acetyltransferase
    Epigenetic Reader Domain

EML 425 

Cat. No.: HY-110263
Handling Instructions

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.

For research use only. We do not sell to patients.

EML 425 Chemical Structure

EML 425 Chemical Structure

CAS No. : 1675821-32-5

Size Price Stock
5 mg USD 110 Get quote
10 mg USD 190 Get quote
25 mg USD 410 Get quote

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.

IC50 & Target[1]

p300

1.1 μM (IC50)

CBP

2.9 μM (IC50)

In Vitro

EML 425 (EML425, Compound 7h) is a potent and selective reversible inhibitor of CBP/p300, noncompetitive versus both acetyl-CoA and a histone H3 peptide, and endows with 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 induces a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9 in U937 cells. 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. The best scoring docking poses suggest that the binding site for EML 425 is an alternative pocket lying near the substrate lysine binding groove and close to the acetylation site[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2702 mL 11.3510 mL 22.7020 mL
5 mM 0.4540 mL 2.2702 mL 4.5404 mL
10 mM 0.2270 mL 1.1351 mL 2.2702 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

To explore the mechanisms of p300 inhibition by EML 425, reactions are performed. Each assay containing 5 nM p300, 3 μM Acetyl CoA, and 50 nM biotinylated H3 (1-21) peptide in 10 μL of assay buffer (50 mM Tris-HCl, pH 8.0, 0.1 mM EDTA, 1 mM DTT, 0.01% Tween-20, 0.01% BSA, 330 nM TSA) is incubated at room temperature for 15 min in a White opaque OptiPlate-384. Reactions are stopped by adding garcinol (final concentration 50 μM) and antiacetyl histone H3 lysine 9 (H3K9Ac) acceptor beads (final concentration 20 μg/mL). After 60 min of incubation at room temperature, 20 μg/mL final concentration of Alpha Streptavidin Donor beads are added in subdued light and incubated in the dark for 30 min at room temperature. Signals are read in Alpha mode with a Enspire plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For cell cycle analysis, 500 μL of U937 cells (2.5×105 cells/mL) are seeded in 24-well plastic plates and incubated with 100 μM EML 425 for 72 h. After this period of treatment, 500 μL of hypotonic buffer (33 mM sodium citrate, 0.1% Triton X-100, 50 μg/mL propidium iodide) is added to cell suspensions. Cells are analyzed with a FACScan flow cytometer and quantitative analysis of cell cycle distribution and hypodiploid nuclei is performed using ModFit LT Macintosh software. All the experiments are performed at least in triplicate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

440.49

Formula

C₂₇H₂₄N₂O₄

CAS No.

1675821-32-5

SMILES

O=C(N(C(N(CC1=CC=CC=C1)C/2=O)=O)CC3=CC=CC=C3)C2=C/C4=C(C=C(O)C=C4C)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EML 425
Cat. No.:
HY-110263
Quantity:

EML 425

Cat. No.: HY-110263