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420089-51-6

420089-51-6 structure
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: 2025-08-27 17:55:32
  • 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].
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

[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.

Molecular Formula C18H14F5NO3S
Molecular Weight 419.37
Hazard Codes Xi
RIDADR NONH for all modes of transport
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