Potent, selective and cell permeable reversible dual inhibitor of CBP and p300 (IC50 values 1.1 μM and 2.9 μM, respectively, and practically inactive against the enzymes GCN5 and PCAF), noncompetitive versus both acetyl-CoA and a histone H3 peptide. 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 that of C646 (Axon 1781).

KEYWORDS: EML 425 | supplier | dual CBP/p300 KAT3 inhibitor | EML425 | CAS [1675821-32-5] | Histone | HAT | Inhibitor | Lysine acyltransferase | H4K5 | H3K9 | G0/G1 arrest | hypodiploid nuclei | C646