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- CAS号：
1320288-19-4
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥213.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥695.0 |
| 规格： | 5mg | 产品价格： | ￥495.0 |
| 规格： | 10mg | 产品价格： | ￥928.0 |
| 规格： | 25mg | 产品价格： | ￥1856.0 |
| 规格： | 50mg | 产品价格： | ￥2984.0 |
| 规格： | 100mg | 产品价格： | ￥4256.0 |
Product Introduction
Bioactivity
| 名称 | UNC 0631 |
| 描述 | UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM). |
| 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) |
| 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. |
| 体内活性 | 在MCF7,22RV1和IMR90细胞中,UNC0631显著降低H3K9me2水平。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.19 mM), Sonication is recommended. Ethanol : 5 mg/mL (7.86 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 49 mg/mL (77.05 mM), Sonication is recommended. |
| 关键字 | UNC-0631 | UNC 0631 | PKMT | p53 | KMT1D | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | H3K9me2 | G9a | EHMT1 | chromatin | cell-penetration |
| 相关产品 | XY1 | MRTX-1719 | （Iso）-Flavokawain A | MAK683 | Tazemetostat | iso-Azalansta | SNDX-5613 | EPZ015666 | AMI-1 free acid | MS37452 | MAK-683 hydrochloride | Piribedil |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Histone Modification Compound Library | Chromatin Modification Compound Library | Epigenetics Compound Library | NO PAINS Compound Library | Membrane Protein-targeted Compound Library | High-Efficiency Gene Editing Small Molecule Library | Post-Translational Modification Compound Library |
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，而且它们的结构和反应活性与苯有相似之处，即有不同程度的芳香性，所以称为芳杂环化合物。 一、杂环化合物的分类和命名 杂环化合物可按杂环的骨架分为单杂环和稠杂环。单杂环又按环的大小分为五元杂环和六元杂环；稠杂环按其稠合环形式分为苯稠杂环和稠杂环。如表19-1所示。 杂环化合物的命名主要采用外文译音法，把杂环化合物的英文名称的汉字译音加“口”字旁表示。例如： 呋喃（furan） 吡啶（pyridine） 外文译音法是根据国际
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 UNC0631【1320288-19-4】
￥213 - 4256
