Biological Activity:

EML425 is a selective, noncompetitive and cell permeable KAT3 histone acetyltransferases CBP/p300 inhibitor with IC50 of 1.1 µM for CBP and 2.9 µM for p300. It is noncompetitive versus both acetyl-CoA and a histone H3 peptide, and endowed with good cell permeability. In human leukemia U937 cells, 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. EML425 may be an invaluable chemical probe not only for mechanistic studies of p300-mediated lysine acetylation but also to further investigate the biological role of this KAT enzyme and its implications in physiological and/or pathological processes.

How to Use:

In vitro: EML425 was used at 10-100 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Milite C, et al. A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach. (2015) J Med Chem. 58(6):2779-98.