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UNC0638

UNC0638

产品编号 T3257   CAS 1255580-76-7

UNC0638 是 β-蛋白赖氨酸甲基转移酶 G9a 和 GLP 的抑制剂,选择性抑制表观遗传和非表观遗传靶标。

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UNC0638 Chemical Structure
UNC0638, CAS 1255580-76-7
规格 价格/CNY 货期 数量
1 mg ¥ 222 现货
5 mg ¥ 494 现货
10 mg ¥ 756 现货
25 mg ¥ 1,418 现货
50 mg ¥ 2,530 现货
100 mg ¥ 3,790 待询
1 mL * 10 mM (in DMSO) ¥ 564 现货
产品目录号及名称: UNC0638 (T3257)
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纯度: 99.53%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
靶点活性 G9a:<15 nM, GLP:19 nM
体外活性 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP, with a toxicity/function ratio of >100, compared to <6 for BIX01294. UNC0638 is a selectivite inhibitor of G9a and GLP over a wide range of epigenetic and non-epigenetic targets. UNC0638 is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. In MDA-MB-231 cells, UNC0638 (48 h exposure) reduces H3K9me2 levels in a concentration-dependent manner with an IC50 of 81 nM. UNC0638 treatment of a variety of cell lines results in lower global H3K9me2 levels, equivalent to levels observed for small hairpin RNA knockdown of G9a and GLP with the functional potency of UNC0638 being well separated from its toxicity. UNC0638 markedly reduces the clonogenicity of MCF7 cells, reduces the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs. In mouse embryonic stem cells, UNC0638 reactivates G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation. [1]
激酶实验 The enzymatic reactions are conducted in duplicate at room temperature for 1 hour in a 50 μL mixture containing PKMT assay buffer, substrate coated plate, 10 M SAM, a HMT enzyme (EZH2 (800 ng/reaction), MLL (300 ng/reaction), PRMT1 (0.5 ng/reaction), SUV39H1 (75 ng/reaction) and UNC0638 (0-1.25 μM). After enzymatic reactions, 100 μL of first antibody is added to each well and the plate is incubated at room temperature for an additional 1 h. 100 μL of secondary antibody is added to each well and the plate is incubated at room temperature for an additional 30 min. 100 μL of developer reagents are added to wells and luminescence is measured using a BioTek SynergyTM 2 microplate reader. Enzyme activity assays are performed in duplicates at each concentration. The luminescence data are analyzed using the computer software, Graphpad Prism[1].
细胞实验 UNC0638 is dissolved in deuterated DMSO (10 mM) and deuterated Water (90:10 ratio)[1]. 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 grown in the presence or absence of UNC0638 (10 nM, 100 nM, 1 μM, 10 μM, and 100 μM ) for stated amount of time. 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 formazan is solubilized in acidified isopropanol and 1% Triton and absorbance measured at 570 nm, corrected for 650 nm background[1].
分子量 509.73
分子式 C30H47N5O2
CAS No. 1255580-76-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 93 mg/mL (182.4 mM)

Ethanol: 93 mg/mL (182.4 mM)

H2O: 6 mg/mL (11.77 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol / H2O 1 mM 1.9618 mL 9.8091 mL 19.6182 mL 49.0456 mL
5 mM 0.3924 mL 1.9618 mL 3.9236 mL 9.8091 mL
10 mM 0.1962 mL 0.9809 mL 1.9618 mL 4.9046 mL
DMSO / Ethanol 20 mM 0.0981 mL 0.4905 mL 0.9809 mL 2.4523 mL
50 mM 0.0392 mL 0.1962 mL 0.3924 mL 0.9809 mL
100 mM 0.0196 mL 0.0981 mL 0.1962 mL 0.4905 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Vedadi M, et al. Nat Chem Biol, 2011, 7(8), 566-574. 2. Wang J Q, Wang L Y, Li S J, et al. Histone methyltransferase G9a inhibitor-loaded redox-responsive nanoparticles for pancreatic ductal adenocarcinoma therapy[J]. Nanoscale. 2020, 12(29): 15767-15774.

文献引用

1. Wang J Q, Wang L Y, Li S J, et al. Histone methyltransferase G9a inhibitor-loaded redox-responsive nanoparticles for pancreatic ductal adenocarcinoma therapy. Nanoscale. 2020, 12(29): 15767-15774.
Tilorone dihydrochloride Asebotin Naringenin Nitazoxanide D-Pinitol Tulobuterol hydrochloride Cinanserin hydrochloride Aurintricarboxylic acid

相关化合物库

该产品包含在如下化合物库中:
糖代谢化合物库 抗糖尿病库 细胞重编程化合物库 已知活性化合物库 抗感染化合物库 抑制剂库 染色质修饰分子库 抗衰老化合物库 抗COVID-19化合物库 抗病毒库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

UNC0638 1255580-76-7 Autophagy Chromatin/Epigenetic Microbiology/Virology Influenza Virus Histone Methyltransferase inhibit UNC-0638 Inhibitor UNC 0638 inhibitor

 

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