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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- Reinheit: 99.90%
- CAS. Nr.: 420089-51-6
- Formel: C18H14F5NO3S
- Molecular Weight:419.37
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
MIC: 1 μM (Mycobacterium tuberculosis)
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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, 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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CAS. Nr. 420089-51-6
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Appearance Solid
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Molecular Weight 419.37
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)