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ATB107 是吲哚-3-甘油磷酸合酶 (IGPS) 的新型有效抑制剂, 其 KD 值为 3 μM。

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ATB107 Chemical Structure

ATB107 Chemical Structure

CAS No. : 455325-51-6

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATB107 is a novel and potent inhibitor of indole-3-glycerol phosphate synthase (IGPS) with a KD of 3 μM.

IC50 & Target

KD: 3 μM (IGPS)[1]

体外研究
(In Vitro)

The minimum inhibitory concentration (MIC) of ATB107 is 0.1 μg/mL for M. tuberculosis H37Ra. ATB107 also has high activity against M. tuberculosis H37Rv, with an MIC of 0.1 μg/mL. All 50 fully susceptible clinical isolates tested are susceptible to ATB107 at 1 μg/mL; of these, 41 (82%) are susceptible to ATB107 at 0.1 μg/mL. The results also show that 67 (83.8%) multidrug-resistant TB (MDR-TB) isolates are susceptible to ATB107 at 1 μg/mL, and 25 (31.3%) isolates are susceptible to ATB107 at 0.1 μg/mL. Results show that the binding ability of ATB107 is well correlated with its concentrations. At the highest concentration of 200 μg/mL, ATB107 can inhibit cell proliferation, with cell survival of about 60%. With the lower concentration of 50 μg/mL, cell survival is more than 80% for ATB107[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

392.50

Formula

C21H28N8

CAS 号
性状

固体

颜色

Light yellow to khaki

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
Kinase Assay
[1]

The concentration of mIGPS is determined. The substrate CdRP is chemically synthesized, with a yield of 30 mM. Ten microliters of 30 mM CdRP and 10 μL of 1.24 μM IGPS are added to 480 μL of 5 mM 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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 200 μg/mL. After incubation of cells treated with ATB107 for 12 h, 20 μL (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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

ATB107 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ATB107
目录号:
HY-76212
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