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A-196

A-196

产品编号 T4343   CAS 1982372-88-2
别名: A 196

A-196 是一种选择性有效的 SUV420H1和 SUV420H2抑制剂,IC50值分别为 0.025 和 0.144 μM。它是一种 SUV4-20的化学探针,以底物竞争性方式抑制 SUV4-20,用于研究组蛋白甲基转移酶在基因组完整性中的作用。

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A-196 Chemical Structure
A-196, CAS 1982372-88-2
规格 价格/CNY 货期 数量
1 mg ¥ 395 现货
2 mg ¥ 568 现货
5 mg ¥ 913 现货
10 mg ¥ 1,490 现货
25 mg ¥ 2,520 现货
50 mg ¥ 3,760 现货
100 mg ¥ 5,380 现货
1 mL * 10 mM (in DMSO) ¥ 719 现货
产品目录号及名称: A-196 (T4343)
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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 A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
靶点活性 SUV420H2:144 nM, SUV420H1:25 nM
体外活性 A-196 potently inhibits SUV420 h1 and SUV420 h2 at both 1 and 10 μM, but has no activity at either concentration against any of the other PKMTs in the panel, including the other H4K20-modifying enzyme, PR-SET7, and those that utilize H3K4, H3K9, H3K27, and H3K79 as substrates. In cells, A-196 induces a global decrease in H4K20me2 and H4K20me3 and a concomitant increase in H4K20me1, but has no effect on any of the other histone modifications. A-196 inhibits 53BP1 foci formation upon ionizing radiation and reduces NHEJ-mediated DNA-break repair but does not affect the homology-directed repair.
激酶实验 Briefly, Hsp90 from porcine spleen extract is isolated by affinity capture on a purine-affinity media. The Hsp90 loaded media is then challenged with test compound (PF-04929113) at a given concentration, ranging from 0.8 to 500 μM, and the amount of Hsp90 liberated at each concentration is determined. The resulting IC50 values are corrected for the ATP ligand concentration and presented as apparent Kd values.
细胞实验 U2OS cells are seeded on 6-well plates with 3 μM A-196 or DMSO as a control, and incubated for 48 h. The cells are washed once in 1 X PBS and then lysis buffer (20 mM Tris-HCl pH 7.5, 0.5% Triton X-100, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, PMSF, protease inhibitors, benzonase) is added to half the cells to create whole cell extract (WCE). The remaining cells are subjected to sequential cellular fractionation. First the cell pellet is resuspended in hypotonic buffer A (10 mM HEPES pH 7.5, 10 mM KCl, 1.5 mM MgCl2, 0.3 M sucrose, 1 mM DTT and protease inhibitors) and then 0.1% triton X-100 is added. The cells are incubated for 15 min on ice and pelleted by centrifugation at 1,500 g. The supernatant is clarified by centrifugation at max speed and saved as the cytoplasmic fraction. The pellet is resuspended in buffer B (3 mM EDTA, 3 mM EGTA, 1 mM DTT and protease inhibitors) and incubated on ice for 40 min and then centrifuged at 1,500 g for 5 min. The supernatant is clarified and saved as the nucleoplasmic fraction. The pellet is resuspended in lysis buffer and incubated for 5 min at room temperature before being resuspended in 4× loading dye. The final lysate contains the solubilized chromatin fraction.
别名 A 196
分子量 359.25
分子式 C18H16Cl2N4
CAS No. 1982372-88-2

存储

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

溶解度

DMSO: 7.2 mg/mL (20 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 1 mM 2.7836 mL 13.9179 mL 27.8358 mL 69.5894 mL
5 mM 0.5567 mL 2.7836 mL 5.5672 mL 13.9179 mL
10 mM 0.2784 mL 1.3918 mL 2.7836 mL 6.9589 mL
20 mM 0.1392 mL 0.6959 mL 1.3918 mL 3.4795 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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参考文献

1. Bromberg KD,etal.The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.Nat Chem Biol. 2017 Mar;13(3):317-324.
Piribedil UNC 0631 MS049 2HCl (1502816-23-0(free base)) Antiproliferative agent-25 Tazemetostat hydrobromide Amodiaquine lutidinic acid EED226

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 已知活性化合物库 经典已知活性库 抑制剂库 表观遗传库 甲基化化合物库 染色质修饰分子库 细胞重编程化合物库 NO PAINS 化合物库 组蛋白修饰化合物库

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
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% Tween 80
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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

A-196 1982372-88-2 Chromatin/Epigenetic Histone Methyltransferase A196 Inhibitor inhibit A 196 inhibitor

 

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