1675821-32-5
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- CAS号:
- 1675821-32-5
- 英文名:
- EML 425
- 英文别名:
- EML 425;5-[(4-Hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-2,4,6(1H,3H,5H)-pyrimidinetrione;EML425,EML 425,HAT,HATs,Epigenetic Reader Domain,inhibit,Inhibitor,Histone Acetyltransferase,EML-425;2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-[(4-hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-
- 中文名:
- 1675821-32-5
- 中文别名:
- 化合物EML 425;EML 425,CBP / P300抑制剂
- CBNumber:
- CB83146291
- 分子式:
- C27H24N2O4
- 分子量:
- 440.49
- MOL File:
- 1675821-32-5.mol
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1675821-32-5化学性质
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沸点:
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622.8±65.0 °C(Predicted)
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密度:
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1.321±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 40 mg/ml
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形态:
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A solid
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酸度系数(pKa):
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8.90±0.40(Predicted)
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1675821-32-5性质、用途与生产工艺
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。
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p300
1.1 μM (IC
50
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CBP
2.9 μM (IC
50
)
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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.
1675821-32-5
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-110263 | 1675821-32-5
EML 425 | 1675821-32-5 | 10mM * 1mLin DMSO | 1210元 |
| 2024/04/30 | S2977 | 1675821-32-5
EML 425 | 1675821-32-5 | 5mg | 1286.21元 |
1675821-32-5, 1675821-32-5 相关搜索:
- 酶
- EML 425,CBP / P300抑制剂
- 化合物EML 425
- 1675821-32-5
- EML425,EML 425,HAT,HATs,Epigenetic Reader Domain,inhibit,Inhibitor,Histone Acetyltransferase,EML-425
- 2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-[(4-hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-
- 5-[(4-Hydroxy-2,6-dimethylphenyl)methylene]-1,3-bis(phenylmethyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
- EML 425