Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KG-548 是一种ARNT/TACC3干扰剂以及HIF-1α抑制剂。KG-548 通过 ARNT 的 PAS-B 结构域与 TACC3 竞争性结合,直接干扰ARNT/TACC3复合物的形成。ARNT 是芳基烃受体核转运蛋白,也称为 HIF-β。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | ¥ 172 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 189 | 5日内发货 |
产品描述 | KG-548 is an ARNT/TACC3 disruptor as well as a HIF-1α inhibitor. KG-548 directly interferes with the formation of the ARNT/TACC3 complex by competitively binding the ARNT PAS-B domain with TACC3. ARNT is the aryl hydrocarbon receptor nuclear translocator which is also known as HIF-β [1][2]. |
体外活性 | HIF is a heterodimer of two bHLH-PAS (basic Helix Loop Helix-Per-ARNT-Sim) subunits, including a HIF-α paralog (HIF-1α, -2α, -3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β) [1]. KG-548 (0-250 μM; 16 h for over night) exhibits the great reduction of ARNT/CCC complex formation for both coactivators, and also disrupts ARNT2 PAS-B/TACC3 interactions [1]. KG-548 (0-2 mM; 16 h for over night) dose-dependently breaks up the (320 μM) ARNT PAS-B/TACC3 complex in vitro and in cell lysate with an IC 50 value of 25 μM [1]. KG-548 significantly inhibits lactate production of glycolysis on in FaDu hypopharyngeal carcinoma cells [2]. Western Blot Analysis [1] Cell Line: HEK293T cell lysates Concentration: 0, 5, 50, 100, 250, 500 μM and 1 mM, 2 mM Incubation Time: 16 hours Result: Weakened the ARNT/TACC3 interaction from 5 μM to 500 μM dose-dependently, and decreased the protein intense of ARNT associated with immunoprecipitated TACC3 protein by 82% (500 μM), 59% (1 mM), 43% (2 mM), respectively. |
分子量 | 282.15 |
分子式 | C9H4F6N4 |
CAS No. | 175205-09-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
KG-548 175205-09-1 Inhibitor inhibitor inhibit