1. Epigenetics
  2. Histone Methyltransferase
  3. EM127

EM127 (化合物 11c) 是一种具有高选择性、高亲和力和位点特异性的 SMYD3 共价抑制剂 (KD=13 μM)。EM127 能有效地抑制 ERK1/2 磷酸化,降低 SMYD3 靶基因的转录调节。EM127 能够有效地和长时间地削弱甲基转移酶的活性。EM127 可用于癌症,尤其是 SMYD3 阳性肿瘤的研究。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

EM127 Chemical Structure

EM127 Chemical Structure

CAS No. : 1886879-71-5

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
1 mg ¥590
In-stock
5 mg ¥1300
In-stock
10 mg ¥2100
In-stock
25 mg ¥4500
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours[1].

IC50 & Target[1]

SMYD3

 

体外研究
(In Vitro)

EM127 (5 μM; 24, 48, 72 h) shows good anti-proliferative activity in MDA-MB-231and HCT116 cells[1].
EM127 (5 μM; 24, 48, 72 h) attenuates the expression of SMYD3 target genes while does not affect expression when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells[1].
EM127 (1, 3.5, 5 μM; 48, 72 h) decreases ERK1/2 phosphorylation in a dose- and time-dependent manner in HCT116 and MDA-MB-231cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, HCT116 cells
Concentration: 5 μM
Incubation Time: 24, 48, 72 h
Result: Significantly retarded cell proliferation by 48 h.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 3.5, 5 μM
Incubation Time: 48 h
Result: Significantly reduced the expression of CDK2 and C-MET, the known SMYD3 regulated genes.
Attenuated the abundance of mRNAs of the extracellular matrix component fibronectin 1 (FN1) and N-cadherin (N-CAD).

Western Blot Analysis[1]

Cell Line: HCT116, MDA-MB-231cells
Concentration: 1, 3.5, 5 μM
Incubation Time: 48, 72 h
Result: Attenuated ERK1/2 phosphorylation and induced PARP processing at the same concentrations that retarded cell proliferation.
分子量

311.76

Formula

C14H18ClN3O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (80.19 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2076 mL 16.0380 mL 32.0760 mL
5 mM 0.6415 mL 3.2076 mL 6.4152 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2076 mL 16.0380 mL 32.0760 mL 80.1899 mL
5 mM 0.6415 mL 3.2076 mL 6.4152 mL 16.0380 mL
10 mM 0.3208 mL 1.6038 mL 3.2076 mL 8.0190 mL
15 mM 0.2138 mL 1.0692 mL 2.1384 mL 5.3460 mL
20 mM 0.1604 mL 0.8019 mL 1.6038 mL 4.0095 mL
25 mM 0.1283 mL 0.6415 mL 1.2830 mL 3.2076 mL
30 mM 0.1069 mL 0.5346 mL 1.0692 mL 2.6730 mL
40 mM 0.0802 mL 0.4009 mL 0.8019 mL 2.0047 mL
50 mM 0.0642 mL 0.3208 mL 0.6415 mL 1.6038 mL
60 mM 0.0535 mL 0.2673 mL 0.5346 mL 1.3365 mL
80 mM 0.0401 mL 0.2005 mL 0.4009 mL 1.0024 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
EM127
目录号:
HY-151379
需求量: