Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Thiophene-2 (TP2) is a targeted inhibitor of polyketide synthase 13 (Pks13), specifically designed to disrupt mycolic acid biosynthesis. By doing so, it effectively induces rapid cell death in mycobacteria. Thiophene-2 demonstrates notable anti-tuberculosis activity and exhibits a minimum inhibitory concentration (MIC) value of 1 μM against Mycobacterium tuberculosis.
产品描述 | Thiophene-2 (TP2) is a targeted inhibitor of polyketide synthase 13 (Pks13), specifically designed to disrupt mycolic acid biosynthesis. By doing so, it effectively induces rapid cell death in mycobacteria. Thiophene-2 demonstrates notable anti-tuberculosis activity and exhibits a minimum inhibitory concentration (MIC) value of 1 μM against Mycobacterium tuberculosis. |
靶点活性 | Mycobacterium tuberculosis:1 μM (MIC) |
体外活性 | In vitro, TP inhibits fatty acyl-AMP loading onto Pks13. Thiophene-2 (TP2; 0-125 μM) inhibits loading of wild-type Mycobacterium tuberculosis (Mtb) Pks13 (Pks13_WT) in a dose-dependent manner. Thiophene-2 also inhibits palmitic acid (FL C16) loading onto the TP-resistant F79S mutant protein[1]. Thiophene-2 has an IC50 versus monkey kidney Vero cells and human liver carcinoma HepG2 cells of 17.5 and 7.30 μM, respectively. Significant intracellular killing activity within BCG-infected J774A.1 macrophage cells is observed at Thiophene-2 concentrations of 12.8 μM[1]. |
别名 | Thiophene-2, TP2 |
分子量 | 419.37 |
分子式 | C18H14F5NO3S |
CAS No. | 420089-51-6 |
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。
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