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

Dihydrofolate reductase (DHFR)

Dihydrofolate reductase (DHFR) catalyzes the reduction of dihydrofolate to tetrahydrofolate using NADPH, and it is involved in the synthesis of nucleotide, in both prokaryotic and eukaryotic cells. DHFR inhibitors are commonly used for fighting malaria and other protozoal infections, as well as for treating fungal, bacterial, and mycobacterial infections.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    Trimetrexate isethionate
  • 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.
    Trimetrexate trihydrochloride
  • HY-10824B
    Talotrexin ammonium
    		Inhibitor
    Talotrexin ammonium is a nonpolyglutamatable antifolate. Talotrexin ammonium improves antitumor activity in a broad spectrum of cancer models by targeting DHFR to inhibit tumor growth.
    Talotrexin ammonium
  • HY-162358
    DHFR-IN-17
    		Inhibitor
    DHFR-IN-17 (compound j9) is an oral active SaDHFR inhibitor with the IC50 of 0.97 nM. DHFR-IN-17 shows antibacterial activity against S. aureus with the minimum inhibitory concentration of 0.031 μg/mL.
    DHFR-IN-17
  • 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.
    EGFR/HER2/DHFR-IN-3
  • HY-168648
    DNA Gyrase/DHFR-IN-1
    		Inhibitor
    DNA Gyrase/DHFR-IN-1 is a dual inhibitor of bacterial DNA gyrase and DHFR, with IC50s of 182 μM and 3.90 μM for E. coli DNA gyrase and DHFR respectively. DNA Gyrase/DHFR-IN-1 has bactericidal and antifungal activity.
    DNA Gyrase/DHFR-IN-1
  • 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).
    DHFR-IN-9
  • HY-163722
    EGFR/DHFR-IN-1
    		Inhibitor
    EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR with IC50s of 0.151 and 0.541 µM, respectively. EGFR/DHFR-IN-1 arrests the cell cycle at both G0-G1 and S phases.
    EGFR/DHFR-IN-1
  • 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.
    DHFR-IN-8
  • HY-121927
    Mobiletrex
    		Inhibitor
    Mobiletrex is an anti folate and dihydrofolate reductase inhibitor that can be used in research on rheumatoid arthritis.
    Mobiletrex
  • 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.
    EGFR/HER2/DHFR-IN-2
  • HY-162475
    Fluorofolin
    		Inhibitor
    Fluorofolin is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.5 nM. Fluorofolin exhibits significant activity against P. aeruginosa.
    Fluorofolin
  • HY-121256
    Chlorasquin
    		Activator
    Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.
    Chlorasquin
  • HY-124350R
    10-Formylfolic acid (Standard)
    		Inhibitor
    10-Formylfolic acid (Standard) is the analytical standard of 10-Formylfolic acid. This product is intended for research and analytical applications. 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
    10-Formylfolic acid (Standard)
  • HY-10824A
    Talotrexin monoammonium
    		Inhibitor
    Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin monoammonium
  • HY-169790
    Phomarin
    		Inhibitor
    Phomarin is an inhibitor for dihydrofolate reductase (DHFR), and exhibits potential antimalarial activity.
    Phomarin
  • 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.
    DHFR-IN-15
  • HY-159899
    DHFR-IN-22
    		Inhibitor
    DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase) inhibitor belonging to the class of 2,4-diaminopyrimidine compounds. DHFR-IN-22 exhibits significant inhibitory activity against purified DHFR enzyme and major species of nontuberculous mycobacteria (NTM), namely Mycobacterium avium and Mycobacterium abscessus. It shows an IC50 of 1.1 nM and MIC of 1.5 μg/mL against M. abscessus, and an IC50 of 6.3 nM and MIC of 0.1 μg/mL against M. avium. Additionally, it demonstrates an IC50 of 2100 nM against human DHFR. DHFR-IN-22 holds potential for studying novel strategies to combat NTM infections.
    DHFR-IN-22
  • 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.
    10-Formylfolic acid
  • 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.
    DHFR-IN-13
Cat. No. Product Name / Synonyms Application Reactivity