MilliporeSigma™ Calbiochem™MycobacteriumBactericide, TCA1

Description

• A cell-permeable benzothiazolylthiophene that exhibits bactericidal activity against mycobacteria, including M
• smegmatis , M
• bovis GCG , and M
• tuberculosis (MIC 50 = 30, 40, and 10 ng/mL, respectively, in biofilm medium; MIC 50 = 4.5, 3, 0.19μg/mL, respectively, in 7H9 medium), but not E
• coli , Staphylococcus aureus , or Pseudomonas aeruginosa , by simultaneously targeting DprE1 FAD-binding domain of DprE1/DprE2 required for Mycobacterium cell wall arabinan biosynthesis and the Mtb MoeW protein involved in the biosynthesis of MoCo, molybdenum cofactor indispensable for nitrate assimilation via MoCo-dependent enzymes
• Either alone or used in combination, TCA1 is shown to greatly complement INH (Isoniazid) and RIF (Rifampicin) against both wt and drug-resistant Mtb cultures in vitro (1-7.5μg/mL) and in treating acute and chronic Mtb H37Rv infections in mice in vivo (10-100mg/kg p.o.) with no apparent host toxicity.