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EML425

Chemical Structure : EML425

CAS No.: 1675821-32-5

EML425 (EML-425)

Catalog No.: PC-22924Not For Human Use, Lab Use Only.

EML425 is a potent, selective, cell-permeable and reversible inhibitor of KAT3 histone acetyltransferases (CBP and p300) with IC50 of 1.1 and 2.9 uM respectively.

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Biological Activity

EML425 is a potent, selective, cell-permeable and reversible inhibitor of KAT3 histone acetyltransferases (CBP and p300) with IC50 of 1.1 and 2.9 uM respectively.
EML425 is inactive against the enzymes GCN5 and PCAF.
EML425 (50-100 uM) induced a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9 in human leukemia U937 cells, a marked arrest in the G0/G1 phase.
EML425 is more potent and selective than curcumin and anacardic acid, with a potency comparable to that of C646.
EML425 is an invaluable chemical probe not only for mechanistic studies of p300-mediated lysine acetylation but also to further investigate the biological role of KAT3 enzymes.

Physicochemical Properties

M.Wt 440.50
Formula C27H24N2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-[(4-Hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-2,4,6(1H,3H,5H)-pyrimidinetrione

References

1. Milite C, et al. J Med Chem. 2015 Mar 26;58(6):2779-98.

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