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)^[1].

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.

DHFR-IN-26 (compound 4d) (5 mg/kg, 10 mg/kg, 20 mg/kg, and 50 mg/kg; i.p.; a single dose) has a high safety profile in BALB/c mice, with an LD₅₀ of 17.39 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

343.31

C₁₇H₁₂F₃N₅

NC1=C2C(C=CC3=C2C=CN3CC4=CC(F)=C(F)C(F)=C4)=NC(N)=N1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. He W, et al. A dual-targeting antimicrobial agent: Discovery and mechanism of action of a novel 7H-Pyrrolo[3,2-f]quinazoline-1,3-diamine compound. Bioorg Chem. 2026 Mar;170:109471.  [Content Brief]