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ATB107  ≥98%

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产品描述：基本信息 产品编号： A11721 产品名称： ATB107 CAS: 455325-51-6   储存条件 粉末 -20℃ 四年     分子式： C21H28N8 溶于液体 -80℃ 六个月 分子量 392.50 -20℃ 一个月 化学名：  (Z)-N-phenyl-4-(piperidin-1-yl)-6-(2-(quinuclidin-3-ylidene)hydrazinyl)-1,3,5-triazin-2-amine   生物活性 产品描述 一种吲哚-3-甘油磷酸合酶 (IGPS) 的新型有效抑制剂, 其 KD 值为 3μM。 靶点 KD: 3μM (IGPS) 体外研究 The minimum inhibitory concentration (MIC) of ATB107 is 0.1μg/mL for M. tuberculosis H37Ra. ATB107 also has high activity against M. tuberculosis H37Rv, with an MIC of 0.1μg/mL. All 50 fully susceptible clinical isolates tested are susceptible to ATB107 at 1μg/mL; of these, 41 (82%) are susceptible to ATB107 at 0.1μg/mL. The results also show that 67 (83.8%) multidrug-resistant TB (MDR-TB) isolates are susceptible to ATB107 at 1μg/mL, and 25 (31.3%) isolates are susceptible to ATB107 at 0.1μg/mL. Results show that the binding ability of ATB107 is well correlated with its concentrations. At the highest concentration of 200μg/mL, ATB107 can inhibit cell proliferation, with cell survival of about 60%. With the lower concentration of 50μg/mL, cell survival is more than 80% for ATB107   推荐实验方法(仅供参考) Kinase Assay The concentration of mIGPS is determined. The substrate CdRP is chemically synthesized, with a yield of 30mM. Ten microliters of 30mM CdRP and 10μL of 1.24μM IGPS are added to 480μL of 5mM Tris/HCl (pH 7.0), and incubated at 37°C for 20 min. The enzyme activity is measured with a spectrophotometer by following the increase in absorbance of the solution at 280 nm. ATB107 is added to the assay mixture to obtain concentrations of 10-4 M, 7.5×10-5 M, 5×10-5 M, 2.5×10-5 M, and 10-5 M, respectively     Cell Assay The tetrazolium dye reduction assay [3-[4,5-dim-ethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT)] is used to determine the effect of ATB107 on cell survival and growth. At first, the THP-1 macrophage cells are inoculated at 8×104 cells/mL) into 96-well plates and incubated at 37°C in a 5% CO2/95% air atmosphere for 24 h. ATB107 is added to give concentrations of 50,100, 150 and 200μg/mL. After incubation of cells treated with ATB107 for 12 h, 20μL (5 g/L) of MTT solution is added to each well; this is followed by incubation for another 4 h to allow the formation of formazan crystals. Finally, 10% SDS is added to dissolve the formazan crystals, and the plates are read on a microplate reader at 570 nm. Controls are included in which only culture media are added to wells containing cells
保存条件：-20℃

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