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

Name	EML 425
Synonyms	EML 425 5-[(4-Hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-2,4,6(1H,3H,5H)-pyrimidinetrione 2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-[(4-hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-
CAS	1675821-32-5

Molecular Formula	C27H24N2O4
Molar Mass	440.49
Storage Condition	Room Temprature
In vitro study	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 (IC 50 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 binding groove and close to the acetylation site.

biological activity

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor. The IC50 was 2.9 and 1.1 μm.

Last Update：2024-04-09 20:52:54

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Product Name: EML 425 Visit Supplier Webpage Request for quotation
CAS: 1675821-32-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-[(4-hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)- Request for Quotation