| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H24N2O4 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
EML 425 is a potent, selective inhibitor of CREB binding protein (CBP) and p300, with IC50 values of 2.9 μM and 1.1 μM, respectively. The manufacturer groups it under its Epigenetics pathway category. It is supplied as a light yellow to yellow solid (C27H24N2O4, MW 440.49) at 98.04% purity.
Physical & Chemical Properties
| CAS Number | 1675821-32-5 |
|---|---|
| Molecular Formula | C27H24N2O4 |
| Molecular Weight | 440.49 g/mol |
| Purity | 98.04% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| 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 |
| Signaling Pathway | Epigenetics |
| Solubility | In Vitro: DMSO: ≥ 250 mg/mL (567.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 1.1 μM (p300), 2.9 μM (CBP)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 250 mg/mL (567.55 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (4.72 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
EML 425 (EML425) is a potent, selective, reversible CBP/p300 inhibitor that is noncompetitive versus both acetyl-CoA and a histone H3 peptide and has good cell permeability. It inhibits p300 and CBP with IC50 values of 2.9 and 1.1 μM, respectively, and is practically inactive against the enzymes GCN5 (general control non derepressible-5) and PCAF (p300/CBP-associated factor). In U937 cells, EML 425 causes a marked, time-dependent decrease in the acetylation of lysine H4K5 and H3K9. EML 425 behaves as a reversible inhibitor that is noncompetitive versus both acetyl-CoA and a histone H3 peptide, and it can bind the free enzyme as well as the enzyme-substrate complex, even with unequal affinity constants. Docking poses with the best scores suggest that EML 425 binds at an alternative pocket adjacent to the substrate lysine binding groove, next to the acetylation site[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Run reactions to examine how EML 425 inhibits p300. Prepare each assay in a White opaque OptiPlate-384 with 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) holding 5 nM p300, 3 μM Acetyl CoA, and 50 nM biotinylated H3 (1-21) peptide, and incubate for 15 min at room temperature. Stop the reactions by adding garcinol (final concentration 50 μM) together with acceptor beads directed against antiacetyl histone H3 lysine 9 (H3K9Ac) (final concentration 20 μg/mL). Incubate for 60 min at room temperature, then add Alpha Streptavidin Donor beads at a final concentration of 20 μg/mL under subdued light and keep the plate in the dark for 30 min at room temperature. Read signals in Alpha mode on an Enspire plate reader[1].
Cell Assay[1]
For cell cycle analysis, seed 500 μL of U937 cells (2.5×105 cells/mL) in 24-well plastic plates and incubate with 100 μM EML 425 for 72 h. After treatment, add 500 μL of hypotonic buffer composed of 33 mM sodium citrate, 0.1% Triton X-100 and 50 μg/mL propidium iodide to the cell suspensions. Analyze the cells with a FACScan flow cytometer, and carry out quantitative analysis of cell cycle distribution and hypodiploid nuclei with ModFit LT Macintosh software. Perform all experiments at least in triplicate[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Advanced glycation end products promote intervertebral disc degeneration by transactivation of matrix metallopeptidase genes. Osteoarthritis Cartilage 2024 Feb;32(2):187-199. PMID: 37717904
USP24-dependent stabilization of Runx2 recruits a p300/NCOA3 complex to transactivate ADAMTS genes and promote degeneration of intervertebral disc in chronic inflammation mice. Biol Direct 2023 Jul 6;18(1):37. PMID: 37415159
