Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平,IC50为 25 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 392 | 现货 | ||
2 mg | ¥ 558 | 现货 | ||
5 mg | ¥ 888 | 现货 | ||
10 mg | ¥ 1,530 | 现货 | ||
25 mg | ¥ 3,290 | 现货 | ||
50 mg | ¥ 4,870 | 现货 | ||
100 mg | ¥ 6,950 | 现货 | ||
500 mg | ¥ 13,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,230 | 现货 |
产品描述 | UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM). |
靶点活性 | G9a:4 nM |
体内活性 | 在MCF7,22RV1和IMR90细胞中,UNC0631显著降低H3K9me2水平。 |
激酶实验 | SAHH-coupled assays: This assay utilizes SAHH to hydrolyze the methyltransfer product SAH to homocysteine and adenosine in the presence of adenosine deaminase which converts adenosine to inosine. The homocysteine concentration is then determined through conjugation of its free sulfhydryl moiety to a thiol-sensitive fluorophore, ThioGlo. For IC50 determinations, assay mixtures are prepared in 25 mM potassium phosphate buffer pH 7.5, 1 mM EDTA, 2 mM MgCl2, 0.01% Triton X-100 with 5 μM SAHH, 0.3 U/mL of adenosine deaminase, 25 μM SAM, and 15 μM ThioGlo. G9a, GLP, SETD7, SETD8, PRMT3 and SUV39H2 are assayed at 25 nM, 100 nM, 200 nM, 250 nM, 500 nM and 100 nM, respectively. Inhibitors are added at concentrations ranging from 4 nM to 16 μM. After 2 min incubation, reactions are initiated by addition of the histone peptides: 10 μM H3(1–25) for G9a, 20 μM H3(1–25) for GLP, 100 μM H3(1–25) for SETD7, 500 μM H4(1–24) for SETD8, 10 μM H4(1–24) for PRMT3 and 200 μM H3K9Me1 (1–15) for SUV39H2. The methylation reaction is followed by monitoring the increase in fluorescence using Biotek Synergy2 plate reader with 360/40 nm excitation filter and 528/20 nm emission filter for 20 min in 384 well-plate format. Activity values are corrected by subtracting background caused by the peptide or the protein. IC50 values are calculated using Sigmaplot. Standard deviations are calculated from two independent experiments. |
细胞实验 | MDA-MB-231, PC3, HCT116 cells are cultured in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Cells are treated with inhibitors for 48 h. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1 mg/mL of MTT and incubated for 1–2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazanis solubilized in acidified isopropanol and 1% Triton. Formazan signal absorbance is measured at 570 nm and corrected for the 650 nm background. IC50s are calculated using GraphPad Prizm statistical package with sigmoidal variable slope dose response curve fit.(Only for Reference) |
别名 | UNC0631 |
分子量 | 635.93 |
分子式 | C37H61N7O2 |
CAS No. | 1320288-19-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 5 mg/mL (7.86 mM), Heating is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 100 mg/mL (157.25 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.5725 mL | 7.8625 mL | 15.725 mL | 39.3125 mL |
5 mM | 0.3145 mL | 1.5725 mL | 3.145 mL | 7.8625 mL | |
DMSO | 10 mM | 0.1573 mL | 0.7863 mL | 1.5725 mL | 3.9313 mL |
20 mM | 0.0786 mL | 0.3931 mL | 0.7863 mL | 1.9656 mL | |
50 mM | 0.0315 mL | 0.1573 mL | 0.3145 mL | 0.7863 mL | |
100 mM | 0.0157 mL | 0.0786 mL | 0.1573 mL | 0.3931 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。
UNC 0631 1320288-19-4 Chromatin/Epigenetic Histone Methyltransferase H3K9me2 p53 UNC-0631 chromatin inhibit EHMT1 G9a KMT1D cell-penetration PKMT Inhibitor UNC0631 inhibitor