DHFR-IN-26
DHFR-IN-26 is an Escherichia coli dihydrofolate reductase (ecDHFR) inhibitor with an IC50 of 0.75 nM. DHFR-IN-26 exerts broad-spectrum antibacterial activity. DHFR-IN-26 disrupts folate metabolism, nucleotide synthesis, and bacterial amino acid metabolic pathways. DHFR-IN-26 disrupts bacterial inner membranes, inhibited biofilm formation, and attenuated phage-related processes. DHFR-IN-26 shows lower toxicity to non-cancerous cells. DHFR-IN-26 can be used for the research of bacterial infections (including infections caused by methicillin-resistant Staphylococcus aureus, multidrug-resistant Escherichia coli, multidrug-resistant Pseudomonas aeruginosa, and lysogenic bacteria).
For research use only. We do not sell to patients.
- Formula: C17H12F3N5
- Molecular Weight:343.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
DHFR-IN-26 (compound 4d) (24 h) displays broad-spectrum antibacterial activity against gram-positive (including MRSA) and gram-negative (including MDR) bacterial strains with MIC values ranging from 0.0625 to 4 μg/mL[1].
DHFR-IN-26 (0.3-100 μM; 24 h) exhibits lower cytotoxicity against human normal LO2 cells (IC50 = 124.4 μM) than 5-Fluorouracil (HY-90006) (IC50 = 111.31 μM) and higher cytotoxicity against Hela cells than 5-Fluorouracil[1].
DHFR-IN-26 (4×, 8× MIC; sampled at 0 h, 30 min, 1 h, 2 h, 4 h, 6 h, 24 h) exhibits bactericidal efficacy against S. aureus CMCC 25923 and E. coli CMCC 25922[1].
DHFR-IN-26 (Concentrations tested to determine biofilm inhibition; 24 h) potently inhibits biofilm formation by S. aureus and E. coli with complete inhibition at 0.5 μg/mL (S. aureus) and 8 μg/mL (E. coli)[1].
DHFR-IN-26 (1×, 2×, 4×, 8×, 16× MIC; 30 min) disrupts the inner membrane permeability of E. coli CMCC 25922, with maximum effect at 2× MIC[1].
DHFR-IN-26 (0.5×, 1×, 2×, 4×, 8× MIC; 6 h) disrupts the E. coli cell membrane, leading to dose-dependent leakage of DNA and proteins[1].
DHFR-IN-26 (1 μg/mL (lysogen growth/phage release); 0, 0.5×, 1×, 2× MIC (adhesion); 12 h (lysogen growth/phage release), 30 min (adhesion)) attenuates lysogen growth, blocks progeny phage release, and reduces host cell adhesion capacity of lysogenic bacteria[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human normal LO2 cells, human cancer Hela cells
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Concentration:0.3-100 μM
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Incubation Time:24 h
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Result:Exhibited an IC50 of 124.4 μM against LO2 cells and an IC50 of 69.75 μM against Hela cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 343.31
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Formula C17H12F3N5
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SMILES
NC1=C2C(C=CC3=C2C=CN3CC4=CC(F)=C(F)C(F)=C4)=NC(N)=N1
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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)
- DHFR-IN-26
- Dihydrofolate reductase (DHFR)
- Bacterial
- Escherichia coli
- multidrug-resistant pseudomonas aeruginosa
- nucleotide synthesis
- Escherichia coli dihydrofolate reductase
- multidrug-resistant escherichia coli
- lysogenic bacteria
- gram-positive bacterial strains
- ecDHFR
- methicillin-resistant staphylococcus aureus
- folate metabolism
- Inhibitor
- inhibitor
- inhibit