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GSK138

Chemical Structure : GSK138

CAS No.:

GSK138 (GSK3081138A)

货号: PC-23207Not For Human Use, Lab Use Only.

GSK138 (GSK3081138A) is a potent, direct inhibitor of M. tuberculosis InhA with IC50 of 0.04 uM, and MIC of 1 uM against M. tuberculosis H37Rv.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GSK138 (GSK3081138A) is a potent, direct inhibitor of M. tuberculosis InhA with IC50 of 0.04 uM, and MIC of 1 uM against M. tuberculosis H37Rv.
GSK138 shows activity against intracellular bacteria growing inside THP-1-derived macrophages in vitro (MIC 0.9 µM).
GSK138 shows no effect up to the highest concentration tested (200 µM) in the cell health assay.
GSK138 shows activity against a set of drug-susceptible, MDR, and extensively drug-resistant (XDR) M.tb clinical isolates with MIC of 3.75 uM.
GSK138 shows activity in acute mouse infection model of TB. 

物理化学性质&存储条件

分子量 433.57
分子式 C17H19N7OS3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-(5-((5-methyl-1-((2-methylthiazol-4-yl)methyl)-1H-pyrazol-3-yl)amino)-1,3,4-thiadiazol-2-yl)-1-(4-methylthiazol-2-yl)ethan-1-ol

参考文献

1. Encinas L, et al. Antimicrob Agents Chemother. 2024 Sep 30:e0035724.

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