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EML 425
CAS No. 1675821-32-5
EML 425 ( —— )
产品货号. M22069 CAS No. 1675821-32-5
EML 425 是一种有效的选择性 CREB 结合蛋白 (CBP)/p300 抑制剂（IC50 分别为 2.9 和 1.1 μM）。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥721 | 有现货 |
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| 10MG | ￥1256 | 有现货 |
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| 25MG | ￥2722 | 有现货 |
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| 50MG | ￥4074 | 有现货 |
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| 100MG | ￥5929 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称EML 425
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述EML 425 是一种有效的选择性 CREB 结合蛋白 (CBP)/p300 抑制剂（IC50 分别为 2.9 和 1.1 μM）。
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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). 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.
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体外实验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 binding groove and close to the acetylation site.
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体内实验——
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同义词——
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通路Chromatin/Epigenetic
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靶点Epigenetic Reader Domain
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受体p300|CBP
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研究领域——
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适应症——
化学信息
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CAS Number1675821-32-5
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分子量440.49
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分子式C27H24N2O4
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纯度>98% (HPLC)
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溶解度DMSO:250 mg/mL (567.55 mM)
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SMILESCC1=CC(O)=CC(C)=C1C=C1C(=O)N(CC2=CC=CC=C2)C(=O)N(CC2=CC=CC=C2)C1=O
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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.
