Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EM127 是一种具有高选择性和有效性的 SMYD3 共价抑制剂,KD 值为 13 μM。EM127 对 ERK1/2 磷酸化有抑制作用,抑制 SMYD3 靶基因的转录调节。EM127 能够在长时间内缓慢减少甲基转移酶的活性。EM127 具有潜在的抗癌活性,可用于研究 SMYD3 阳性肿瘤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 652 | 现货 | ||
5 mg | ¥ 1,080 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,730 | 现货 | ||
50 mg | ¥ 5,990 | 现货 | ||
100 mg | ¥ 7,910 | 现货 |
产品描述 | EM127 is a highly selective and potent covalent inhibitor of SMYD3 with a KD value of 13 μM.EM127 inhibits ERK1/2 phosphorylation and inhibits transcriptional regulation of SMYD3 target genes.EM127 slowly reduces methyltransferase activity over a long period of time.EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors. EM127 has potential anticancer activity and can be used to study SMYD3 positive tumors. |
体外活性 | In MDA-MB-231 and HCT116 cells, EM127 exhibits good anti-proliferative activity when treated with 5 μM for 24, 48, and 72 hours[1]. Additionally, at the same concentration and time points, EM127 diminishes the expression of SMYD3 target genes. However, this effect is not observed when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells[1]. Furthermore, in both HCT116 and MDA-MB-231 cells, EM127, at concentrations of 1, 3.5, and 5 μM for 48 and 72 hours, decreases ERK1/2 phosphorylation in a dose- and time-dependent manner[1]. |
分子量 | 311.76 |
分子式 | C14H18ClN3O3 |
CAS No. | 1886879-71-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (64.15 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2076 mL | 16.038 mL | 32.076 mL | 80.1899 mL |
5 mM | 0.6415 mL | 3.2076 mL | 6.4152 mL | 16.038 mL | |
10 mM | 0.3208 mL | 1.6038 mL | 3.2076 mL | 8.019 mL | |
20 mM | 0.1604 mL | 0.8019 mL | 1.6038 mL | 4.0095 mL | |
50 mM | 0.0642 mL | 0.3208 mL | 0.6415 mL | 1.6038 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
EM127 1886879-71-5 Chromatin/Epigenetic MAPK Histone Methyltransferase ERK Inhibitor inhibitor inhibit