420089-51-6
420089-51-6 structure
- Name: TP2
- Chemical Name: Thiophene-2
- CAS Number: 420089-51-6
- Molecular Formula: C18H14F5NO3S
- Molecular Weight: 419.37
- Catalog: Signaling Pathways Anti-infection Bacterial
- Create Date: 2020-08-11 12:49:42
- Modify Date: 2024-01-10 19:57:55
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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].
| Name | Thiophene-2 |
|---|---|
| Synonyms | MFCD01337175 |
| Description | 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]. |
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| Related Catalog | |
| Target |
MIC: 1 μM (Mycobacterium tuberculosis) |
| In Vitro | 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]. |
| References |
| Molecular Formula | C18H14F5NO3S |
|---|---|
| Molecular Weight | 419.37 |
| Hazard Codes | Xi |
|---|---|
| RIDADR | NONH for all modes of transport |