Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EED226 是多梳抑制复合物 2 抑制剂,是一种有效的、选择性的、可口服的胚胎外胚层发育 (EED) 抑制剂,IC50 为 22 nM,具有强抗肿瘤活性。当 H3K27me0 肽用作体外酶法测定的底物时,它抑制 PRC2的 IC50为 23.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 498 | 现货 | ||
10 mg | ¥ 747 | 现货 | ||
25 mg | ¥ 1,258 | 现货 | ||
50 mg | ¥ 1,995 | 现货 | ||
100 mg | ¥ 3,715 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 521 | 现货 |
产品描述 | EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. |
靶点活性 | EED:22 nM |
体外活性 | EED226 induces a conformational change upon binding EED, leading to loss of PRC2 activity. EED226 also effectively inhibits PRC2 containing a mutant EZH2 protein resistant to SAM-competitive inhibitors. It regulates histone H3K27 methylation and PRC2 target gene expression in cells. In the in vitro enzymatic assays, EED226 inhibits PRC2 with an IC50 (half-maximal inhibitory concentration) of 23.4 nM when the H3K27me0 peptide is used as substrate and an IC50 of 53.5 nM when the mononucleosome is used as the substrate, with the stimulatory H3K27me3 added at 1 × Kact (1.0 μM). EED226 is noncompetitive with both SAM and peptide substrate. EED226 bound to EED and PRC2 complex with a 1:1 stoichiometry and Kd of 82 nM and 114 nM, respectively. EED226 does not disrupt the PRC2 complex and could still occupy its binding pocket with a SAM-competitive EZH2 inhibitor bound to PRC2. EED226 shows remarkable selectivity for PRC2 complex over 21 other protein methyltransferases, kinases and other protein classes, The only other histone methyltransferase that can be inhibited by EED226 is the EZH1-PRC2 complex. EED226 with moderate permeability leads to a dose-dependent decrease of both global H3K27me3 and H3K27me2 markers in G401 cell[1]. |
体内活性 | EED226 effectively induces tumor regression in a mouse xenograft model. EED226 in a solid dispersion formulation are well tolerated in animals. EED226 clearly demonstrates a dose-dependent efficacy in the mouse xenograph study[1]. EED226 inhibits the growth of diffuse large B-cell lymphoma (DLBCL) xenografts and reduces H3K27me3 levels to a similar extent as an EZH2 inhibitor[2]. EED226 has very low in vivo and in vitro clearance and approximately 100% oral bioavailability, low volume of distribution (0.8 L/kg), reasonable terminal t1/2 (2.2 h), and moderate plasma protein binding (PPB)(14.4%). Its solubility is relatively low and with little dependency on the pH of the medium[3]. |
细胞实验 | G401 cells are treated with EED226 for 3 d at the indicated concentrations. Total histone H3 is shown as a loading control. WB analysis for protein expression of H3K27me3, H3K27me2, H3K27me1. (Only for Reference) |
分子量 | 369.4 |
分子式 | C17H15N5O3S |
CAS No. | 2083627-02-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 68 mg/mL (184.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7071 mL | 13.5355 mL | 27.0709 mL | 67.6773 mL |
5 mM | 0.5414 mL | 2.7071 mL | 5.4142 mL | 13.5355 mL | |
10 mM | 0.2707 mL | 1.3535 mL | 2.7071 mL | 6.7677 mL | |
20 mM | 0.1354 mL | 0.6768 mL | 1.3535 mL | 3.3839 mL | |
50 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3535 mL | |
100 mM | 0.0271 mL | 0.1354 mL | 0.2707 mL | 0.6768 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。
EED226 2083627-02-3 Chromatin/Epigenetic Histone Methyltransferase inhibit antitumor EED 226 Inhibitor PRC2 EED K27me3 EED-226 inhibitor