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-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.
    WR99210
  • 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.
    Trimetrexate
  • HY-108251
    Methotrexate metabolite
    		Inhibitor 98.44%
    Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.
    Methotrexate metabolite
  • HY-W041498
    4-O-Methyldopamine hydrochloride
    		99.48%
    4-O-Methyldopamine hydrochloride is a catecholamine compound that has an inhibitory effect on dihydropteridine reductase.
    4-O-Methyldopamine hydrochloride
  • 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.
    4′-DTMP
  • HY-W320239
    QDPR-IN-1
    		99.28%
    QDPR-IN-1 (Compound 9b) is a potent QDPR inhibitor with an IC50 of 0.72 μM.
    QDPR-IN-1
  • HY-148994
    Methotrexate-γ-aspartate
    		Inhibitor
    Methotrexate-γ-aspartate is a Ll210 cell dihydrofolate reductase inhibitor. Methotrexate-γ-aspartate is apparently more resistant to enzymic cleavage than is methotrexate-y-glutamate. Methotrexate-γ-aspartate can be used in antibody-targeted liposomes and is promising for research of leukemic.
    Methotrexate-γ-aspartate
  • 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-153007
    DHFR-IN-5
    		Inhibitor 99.27%
    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.
    DHFR-IN-5
  • HY-106434
    Piritrexim
    		Inhibitor
    Piritrexim (BW 301U) is a potent dihydrofolate reductase (DHFR) inhibitor against Pneumocystis carinii and Toxoplasma gondii, with IC50 values of 0.038 and 0.011 μM, respectively. Piritrexim can be used for acquired immune deficiency syndrome (AIDS) research. Piritrexim also is an anticancer agent.
    Piritrexim
  • HY-151159
    DHFR-IN-4
    		Inhibitor 99.19%
    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.
    DHFR-IN-4
  • HY-10824
    Talotrexin
    Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin
  • 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.
    VEGFR-2/DHFR-IN-1
  • 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.
    WR99210 hydrochloride
  • 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.
    Metioprim
  • HY-108251R
    Methotrexate metabolite (Standard)
    		Inhibitor
    Methotrexate metabolite (Standard) is the analytical standard of Methotrexate metabolite. This product is intended for research and analytical applications. 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 (Standard)
  • 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.
    VEGFR-2/DHFR-IN-2
  • HY-116039
    Epiroprim
    		Inhibitor
    Epiroprim (Ro11-8958) is a selective dihydrofolate reductase (DHFR) inhibitor. Epiroprim displays excellent activity against staphylococci, enterococci, pneumococci, and streptococci.
    Epiroprim
  • 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
Cat. No. Product Name / Synonyms Application Reactivity