2. Anti-infection
  3. Bacterial
  4. Thiophene-2

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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Thiophene-2 Chemical Structure

Thiophene-2 Chemical Structure

CAS No. : 420089-51-6

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Based on 1 publication(s) in Google Scholar

Thiophene-2 Related Antibodies

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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].

IC50 & Target

MIC: 1 μM (Mycobacterium tuberculosis)
Cellular Effect
Cell Line Type Value Description References
HeLa IC50
> 25 μM
Compound: 38; MMV461553
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
[PMID: 30647879]
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.

Thiophene-2 Related Antibodies
Clinical Trial
Molecular Weight

419.37

Formula

C18H14F5NO3S
CAS No.
SMILES

O=C(OC)C1=C(SC2=C1CCCCC2)NC(C3=C(C(F)=C(C(F)=C3F)F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Thiophene-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Thiophene-2420089-51-6Thiophene2Thiophene 2BacterialPks13mycolicacidtuberculosismycobacterialbactericidalInhibitorinhibitorinhibit

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