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.
Pack Size | Availability | Price/USD | Quantity |
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5 mg | Inquiry | $ 970.00 |
Description | 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. |
Targets&IC50 | Mycobacterium tuberculosis:1 μM (MIC) |
In vitro | In vitro, TP inhibits the fatty acyl-AMP's ability to bind with Pks13, and Thiophene-2 (TP2; 0-125 μM) demonstrates a dose-dependent inhibition of this activity in both wild-type Mycobacterium tuberculosis (Mtb) Pks13 (Pks13_WT) and the TP-resistant F79S mutant protein, specifically affecting palmitic acid (FL C16) loading. Furthermore, Thiophene-2 exhibits significant cytotoxic activity, with an IC50 of 17.5 μM against monkey kidney Vero cells and 7.30 μM against human liver carcinoma HepG2 cells. Notably, it also shows considerable intracellular killing capacity within BCG-infected J774A.1 macrophage cells at concentrations of 12.8 μM[1]. |
Synonyms | Thiophene-2, TP2 |
Molecular Weight | 419.37 |
Formula | C18H14F5NO3S |
CAS No. | 420089-51-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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