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EML 425
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EML 425图片
CAS NO:1675821-32-5
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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。

产品描述

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

体外活性

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. EML 425, noncompetitive versus both acetyl-CoA and a histone H3 peptide, shows 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 causes a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9 in U937 cells. The binding site for EML 425 is an alternative pocket lying near the substrate lysine binding groove and close to the acetylation site[1].

Cas No.

1675821-32-5

分子式

C27H24N2O4

分子量

440.49

储存和溶解度

DMSO:250 mg/mL (567.55 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years