EML 425 - CAS:1675821-32-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	EML 425
英文名称:	EML 425
CAS No:	1675821-32-5	分子式:	C₂₇H₂₄N₂O₄	分子量:	440.49
CAS No:	1675821-32-5
分子式:	C₂₇H₂₄N₂O₄
分子量:	440.49

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

E10399 EML 425 ≥98% (psaitong)

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包装规格：

5mg in glass bottle

溶解性：

溶于DMSO（≥250mg/mL）

产品描述：

基本信息

产品编号：E10399
产品名称：EML 425
CAS:	1675821-32-5	储存条件	粉末	-20℃	四年

分子式：	C27H24N2O4		溶于液体	-80℃	六个月
分子量：	440.49			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO
		Ethanol
		Water
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.2702mL	11.3510mL	22.7020mL
5mM	0.4540mL	2.2702mL	4.5404mL
10mM	0.2270mL	1.1351mL	2.2702mL

生物活性

产品描述

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。

靶点/IC50

p300
1.1μM (IC50)

CBP
2.9μM (IC50)

体外研究

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 1.1μM,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.

推荐实验方法(仅供参考)

激酶实验：

To explore the mechanisms of p300 inhibition by EML 425, reactions are performed. Each assay containing 5nM p300, 3μM Acetyl CoA, and 50nM biotinylated H3 (1-21) peptide in 10μL of assay buffer (50mM Tris-HCl, pH 8.0, 0.1mM EDTA, 1mM DTT, 0.01% Tween-20, 0.01% BSA,330nM TSA) is incubated at room temperature for 15 min in a White opaque OptiPlate384.Reactions are stopped by adding garcinol (final concentration 50μM) and antiacetyl histone H3 lysine 9 (H3K9Ac) acceptor beads (final concentration 20μg/mL). After 60 min of incubation at room temperature, 20μg/mL final concentration of Alpha Streptavidin Donor beads are added in subdued light and incubated in the dark for 30 min at room temperature. Signals are read in Alpha mode with a Enspire plate reader.

细胞实验:

For cell cycle analysis, 500μL of U937 cells (2.5×105 cells/mL) are seeded in 24-well plastic plates and incubated with 100μM EML 425 for 72 h. After this period of treatment, 500μL of hypotonic buffer (33mM sodium citrate, 0.1% Triton X-100, 5μg/mL propidium iodide) is added to cell suspensions. Cells are analyzed with a FACScan flow cytometer and quantitative analysis of cell cycle distribution and hypodiploid nuclei is performed using ModFit LT Macintosh software. All the experiments are performed at least in triplicate.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

搜索质检报告(COA)

参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果