Thiophene-2
Based on 1 Customer Validation
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.
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- Pureza : 99.90%
- No. CAS: 420089-51-6
- Fòrmula: C18H14F5NO3S
- Peso molecular:419.37
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
MIC: 1 μM (Mycobacterium tuberculosis)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>25 μM
Compound: 38; MMV461553
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
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[PMID: 30647879] |
| HepG2 | IC50 |
7.3 μM
Compound: 1
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Cytotoxicity against human HepG2 cells assessed as reduction in cell growth
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth
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[PMID: 37544185] |
| Vero | IC50 |
17.5 μM
Compound: 1
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
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[PMID: 37544185] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 420089-51-6
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Appearance Solid
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Peso molecular 419.37
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Fòrmula C18H14F5NO3S
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Color White to off-white
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SMILES
O=C(OC)C1=C(SC2=C1CCCCC2)NC(C3=C(C(F)=C(C(F)=C3F)F)F)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Thiophene-2 Related Classifications
HY-117145 Related Classifications
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