| Bioactivity | Thiophene-2 (TP2) is a specific polyketide synthase 13 (Pks13) inhibitor. Thiophene-2 inhibits mycolic acid biosynthesis and rapidly leads to mycobacterial cell death. Thiophene-2 is active against Mycobacterium tuberculosis with a MIC value of 1 μM, and has potent anti-tuberculosis activity[1]. |
| Target | MIC: 1 μM (Mycobacterium tuberculosis) |
| Invitro | In vitro, TP inhibits fatty acyl-AMP loading onto Pks13. Thiophene-2 (TP2; 0-125 μM) inhibits loading of wild-type Mycobacterium tuberculosis (Mtb) Pks13 (Pks13_WT) in a dose-dependent manner. Thiophene-2 also inhibits palmitic acid (FL C16) loading onto the TP-resistant F79S mutant protein[1].Thiophene-2 has an IC50 versus monkey kidney Vero cells and human liver carcinoma HepG2 cells of 17.5 and 7.30 μM, respectively. Significant intracellular killing activity within BCG-infected J774A.1 macrophage cells is observed at Thiophene-2 concentrations of 12.8 μM[1]. |
| Name | Thiophene-2 |
| CAS | 420089-51-6 |
| Formula | C18H14F5NO3S |
| Molar Mass | 419.37 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Regina Wilson, et al. Antituberculosis Thiophenes Define a Requirement for Pks13 in Mycolic Acid Biosynthesis. Nat Chem Biol. 2013 Aug;9(8):499-506. |
Thiophene-2
CAS: 420089-51-6 F: C18H14F5NO3S W: 419.37
Thiophene-2 (TP2) is a specific polyketide synthase 13 (Pks13) inhibitor. Thiophene-2 inhibits mycolic acid biosynthesis
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.