EML425 是一种有效的选择性 CREB 结合蛋白 (CBP)/p300 抑制剂。IC₅₀ 为 2.9 和 1.1 μM。

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC 50 s of 2.9 and 1.1 μM, respectively.

Solid

IC50: 1.1 μM (p300), 2.9 μM (CBP)

EML 425 (EML425, Compound 7h) is a potent and selective reversible inhibitor of CBP/p300, noncompetitive versus both acetyl-CoA and a histone H3 peptide, and endows with good cell permeability. EML 425 inhibits both p300 and CBP (IC50 values of 2.9 and 1.1 μM, respectively) while being practically inactive against the enzymes general control non derepressible-5 (GCN5) and p300/CBP-associated factor (PCAF). EML 425 induces a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9 in U937 cells. EML 425 is shown to be a reversible inhibitor, noncompetitive versus both acetyl-CoA and a histone H3 peptide, and able to bind both the free enzyme and the enzyme-substrate complex, even with unequal affinity constants. The best scoring docking poses suggest that the binding site for EML 425 is an alternative pocket lying near the substrate lysine bindi

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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. J Med Chem. 2015 Mar 26;58(6):2779-98.

In Vitro: DMSO : ≥ 250 mg/mL (567.55 mM)配制储备液