Powder: -20°C for 3 years | In solvent: -80°C for 2 years
PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，对丙酮酸脱氢酶激酶 4有抑制作用，IC50为 84 nM，具有口服活性。它抑制细胞转化和细胞增殖并诱导细胞凋亡。它具有抗过敏，抗糖尿病和抗癌作用。
| 产品描述 | PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4, IC50 value = 84 nM). |
| 靶点活性 | Pyruvate dehydrogenase kinase 4 (PDK4):84 nM |
| 体外活性 | PDK4-IN-1 hydrochloride treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1[1]. PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1[1]. |
| 体内活性 | PDK4-IN-1 (C57BL/6J mice) treatment significantly improves glucose tolerance[1]. Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, |
| 分子量 | 393.87 |
| 分子式 | C22H20ClN3O2 |
| CAS No. | 2310262-11-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 125 mg/mL (317.36 mM), Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
参考文献
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。
计算器bottom
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。
PDK4-IN-1 hydrochloride 2310262-11-2 Apoptosis PI3K/Akt/mTOR signaling PDK inhibit anti-allergic Pyruvate dehydrogenase kinase PDHE1α antidiabetic p53 BCL-xL PARP1 caspase-3 BAX Inhibitor p-Akt PDK4 PDK4 IN 1 hydrochloride PDK4IN1 hydrochloride PDK-4-IN-1 hydrochloride PDHK metabolites PDH kinase anticancer inhibitor
沪公网安备 31010602006700号
