1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Dihydrofolate reductase (DHFR)
  4. Dihydrofolate reductase (DHFR) Inhibitor

Dihydrofolate reductase (DHFR) Inhibitor

Dihydrofolate reductase (DHFR) Inhibitors (25):

Cat. No. Product Name Effect Purity
  • HY-116387
    WR99210
    Inhibitor 98.72%
    WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii.
  • HY-10373
    Trimetrexate
    Inhibitor 99.22%
    Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
  • HY-108251
    Methotrexate metabolite
    Inhibitor 98.22%
    Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent. Methotrexate metabolite is an antimalarial agent, which inhibits the parasite growth with an IC50 of 446 nM against the antifolate-sensitive strain and 812 nM against the highly resistant strain under physiological folate conditions. Methotrexate metabolite is inactive against mammalian cells. Methotrexate metabolite is a minimal inhibitor of dihydrofolate reductase among metabolites of methotrexate .
  • HY-W587663
    4′-DTMP
    Inhibitor
    4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFRWT) and 34.3 nM (DHFRL28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli.
  • HY-151159
    DHFR-IN-4
    Inhibitor
    DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.
  • HY-116039
    Epiroprim
    Inhibitor
    Epiroprim (Ro11-8958) is a selective dihydrofolate reductase (DHFR) inhibitor. Epiroprim displays excellent activity against staphylococci, enterococci, pneumococci, and streptococci.
  • HY-149633
    EGFR/HER2/DHFR-IN-3
    Inhibitor
    EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells.
  • HY-151458
    VEGFR-2/DHFR-IN-1
    Inhibitor
    VEGFR-2/DHFR-IN-1 (compound 8b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.384 and 7.881 μM, respectively. VEGFR-2/DHFR-IN-1 shows good antibacterial activities against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, respectively. VEGFR-2/DHFR-IN-1 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 2.97-7.12 μM. VEGFR-2/DHFR-IN-1 can be used for the research of cancer.
  • HY-116387A
    WR99210 hydrochloride
    Inhibitor
    WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii.
  • HY-122289
    Metioprim
    Inhibitor
    Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria.
  • HY-151459
    VEGFR-2/DHFR-IN-2
    Inhibitor
    VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer.
  • HY-10373B
    Trimetrexate isethionate
    Inhibitor
    Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
  • HY-10373A
    Trimetrexate trihydrochloride
    Inhibitor
    Trimetrexate (CI-898) trihydrochloride is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
  • HY-156123
    DHFR-IN-9
    Inhibitor
    DHFR-IN-9 (compound 8A) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-9 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=0.25 μg/mL) and has anti-infective effects in mouse models of systemic infection and thigh infection caused by it (dose: 2.5 mg /kg, 5 mg/kg; ip). DHFR-IN-9 has stronger anticancer activity than paclitaxel (Y-B0015) in a mouse model of breast cancer (dose: 2.5 mg/kg; ip; once every 3 days).
  • HY-156122
    DHFR-IN-8
    Inhibitor
    DHFR-IN-8 (compound 6r) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-8 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=15.6 ng/mL) in mouse models of systemic infection and thigh infection.
  • HY-153007
    DHFR-IN-5
    Inhibitor
    DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity.
  • HY-149632
    EGFR/HER2/DHFR-IN-2
    Inhibitor
    EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth.
  • HY-161064
    DHFR-IN-15
    Inhibitor
    DHFR-IN-15 (compound 34) is a dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity. DHFR-IN-15 effectively binds to DHFR in cells, reducing DHFR levels to 10 nM.
  • HY-124350
    10-Formylfolic acid
    Inhibitor
    10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
  • HY-161010
    DHFR-IN-13
    Inhibitor
    DHFR-IN-13 (Compd Hit8) is an active R. solani DHFR inhibitor with an IC50 value of 10.2 μM. DHFR-IN-13 has selectivity of inhibition against human DHFR with an IC50 value of 227.7 μM. DHFR-IN-13 also is a fungicide. DHFR-IN-13 has high antifungal activity against R. solani with EC50 value of 38.2 mg/L.