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EML 425
- Soluble in DMSO
- MF: C27H24N2O4
- MW: 440.49
Description
EML 425 is a potent, selective, cell permeable and reversible dual inhibitor of CBP and p300 with IC50 values of 1.1 μM and 2.9 μM, respectively. It showed virtually no activity against the acetyltransferases GCN5 and PCAF, acting noncompetitively with respect to both acetyl-CoA and the histone H3 peptide substrate. EML425 induced a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9, a marked arrest in the G0/G1 phase and a significant increase in the hypodiploid nuclei percentage in human leukemia U937 cells. EML425's potency is comparable to C646 (Axon 1781).
CBP/p300 KAT3 pharmacology is highly relevant to disease-relevant cellular and translational research models; EML 425 supports mechanistic studies of CBP/p300 KAT3 in biochemical, cellular and disease-model assays.
Key Features
- Dual CBP/p300 KAT3 inhibitor (IC50: 1.1 μM and 2.9 μM)
- Practically inactive against GCN5 and PCAF
- Reduces H4K5 and H3K9 acetylation in human leukemia U937 cells
- Induces G0/G1 cell cycle arrest and elevates hypodiploid nuclei levels.
Applications
- CBP/p300 KAT3 pharmacology and target-validation studies
- CBP/p300 KAT3 pathway and signaling assays
- Disease-relevant cellular and translational model systems
- Epigenetic regulation, chromatin and transcriptional profiling
More Information
| Parent CAS No. | 1675821-32-5 |
|---|---|
| Chemical Name | 1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione |
| SMILES | C1(=O)N(CC2=CC=CC=C2)C(=O)/C(=C/C2=C(C)C=C(O)C=C2C)/C(=O)N1CC1=CC=CC=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C27H24N2O4/c1-18-13-22(30)14-19(2)23(18)15-24-25(31)28(16-20-9-5-3-6-10-20)27(33)29(26(24)32)17-21-11-7-4-8-12-21/h3-15,30H,16-17H2,1-2H3 |
| InChiKey | LUGQBJDYUPNAQQ-UHFFFAOYSA-N |
| CID | 91826273 |
| Short Description | dual CBP/p300 KAT3 inhibitor |
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