FabI-IN-1
FabI-IN-1 is a FabI (enoyl-acyl carrier protein reductase) inhibitor with a Ki of 0.32 μM against E. coli FabI. FabI-IN-1 inhibits exhibits activity against Gram-negative bacteria including Escherichia coli (MIC = 6.25 μM) and Klebsiella pneumoniae. FabI-IN-1 rescues Galleria mellonella larvae from lethal Escherichia coli infection. FabI-IN-1 exerts a synergistic effect with Colistin (HY-113678) against Escherichia coli. FabI-IN-1 can be used for the research of gram-negative bacterial infection.
For research use only. We do not sell to patients.
- Formula: C14H14BN3O3S
- Molecular Weight:315.16
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
FabI-IN-1 (Compound 11) (2 μM) potently inhibits recombinant E. coli FabI enzyme with a preliminary Ki of 0.32 μM and achieves 80.3% inhibition at a concentration of 2 μM[1].
FabI-IN-1 (compound 11) (24 h) inhibits the growth of multiple Gram-negative bacterial strains, with MIC values ranging from 6.25 μM to 75 μM[1].
FabI-IN-1 (72 h) exhibits low in vitro cytotoxicity against mammalian cells, with IC50 values of 106 ± 13 μM in HepG2 cells and 240 ± 9 μM in Hs27 cells after 72 h incubation[1].
FabI-IN-1 (1.25-5.01 μM; 24 h) exhibits synergistic antibacterial activity with colistin against E. coli ATCC25922, with an FICI of 0.25, and reduces the MIC of Colistin (HY-113678) by 4-fold at concentrations of 1.25 μM and 5.01 μM[1].
FabI-IN-1 (25 μM; 24 h) at 25 μM (4×MIC) exhibits bactericidal activity against E. coli ATCC25922, eliminating all viable bacteria within 24 h without evidence of resistance development[1].
FabI-IN-1 (200 μM; 48 h) has an MPC of 200 μM against E. coli ATCC25922, and spontaneous resistance mutations occur at a low frequency of 2×10-8 to 9×10-9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human HepG2 hepatocarcinoma cells, human Hs27 normal fibroblast cells
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Concentration:Serial dilutions (IC50 determination)
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Incubation Time:72 h
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Result:Demonstrated an IC50 of 106 ± 13 μM in HepG2 cells.
Demonstrated an IC50 of 240 ± 9 μM in Hs27 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Greater wax moth (final instar larvae, average weight 350 mg, inoculated with Escherichia coli ATCC25922)[1]
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Dosage:0.563 mg/kg; 1.13 mg/kg; 2.81 mg/kg; 5.63 mg/kg
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Administration:Intrahemocoelic injection; single dose; 1 hour post-infection
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Result:Exhibited 70% survival rate at 0.563 mg/kg, which was not statistically significant compared to the nontreated infected group.
Achieved 75% survival rate at 1.13 mg/kg, which was significantly different from the nontreated infected group.
Demonstrated survival efficacy equivalent to Ciprofloxacin (HY-B0356) (20 mg/kg) at 2.81 mg/kg, with no statistically significant difference.
Showed no significant toxic effects relative to the PBS-only injected group up to 72 hours post-treatment at 5.63 mg/kg.
Chemical Information
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Molecular Weight 315.16
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Formula C14H14BN3O3S
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SMILES
OB1N(S(=O)(C2=CC=CC(N)=C2)=O)N=CC3=CC(C)=CC=C13
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)