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-10373
    Trimetrexate
    		Inhibitor 99.60%
    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-116387
    WR99210
    		Inhibitor 99.10%
    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-10824
    Talotrexin
    		99.27%
    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-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-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-160254
    1954U89
    		Inhibitor
    1954U89 is a potent, lipid-soluble and orally active inhibitor of dihydrofolate reductase (DHFR). 1954U89 exhibits anticancer activity.
    1954U89
  • HY-137357
    5-Monobutyl methotrexate
    		Inhibitor
    5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors.
    5-Monobutyl methotrexate
  • HY-185443
    UCP1172
    		Inhibitor
    UCP1172 is an antibacterial (Antibacterial) agent and Dihydrofolate reductase inhibitor, with an IC50 of 0.0089 μM against Staphylococcus aureus DfrB, 0.22 μM against DfrG, 0.41 μM against DfrA, and 0.030 μM against DfrK. UCP1172 potently inhibits the growth of MRSA/MSSA isolates carrying dfrG and dfrK (MIC values of 0.3125-0.625 μg/mL), shows weak activity against MRSA carrying dfrA (MIC of 5 μg/mL), and exerts extremely potent inhibitory effects on wild-type S. aureus ATCC 43300 (MIC of 0.0098 μg/mL). UCP1172 can be used in studies related to tuberculosis and Staphylococcus aureus infections.
    UCP1172
  • HY-W041498
    4-O-Methyldopamine hydrochloride
    		99.46%
    4-O-Methyldopamine hydrochloride is a catecholamine compound that has an inhibitory effect on dihydropteridine reductase.
    4-O-Methyldopamine hydrochloride
  • 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-116387A
    WR99210 hydrochloride
    		Inhibitor 98.34%
    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-106434
    Piritrexim
    		Inhibitor 99.07%
    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-B0921
    Succinylsulfathiazole
    		Inhibitor 99.22%
    Succinylsulfathiazole (Succinylsulphathiazole) is a long-acting sulfonamide antibiotic with localized gut-specific antibacterial activity and is orally active. Succinylsulfathiazole inhibits bacterial folate synthesis, reduces coliform counts, suppresses intestinal bacterial growth and vitamin biosynthesis, and depletes gut folate-producing bacteria. Succinylsulfathiazole modulates hepatic mTOR signaling, diminishes cecal fermentation, decreases hepatic folate levels and total folate excretion, elevates nitrogen excretion and reduces the fermentability of certain dietary fibers. Succinylsulfathiazole induces folate deficiency and triggers biotin- and folate-related nutritional deficiency symptoms in rats and C57BL/6 mice.
    Succinylsulfathiazole
  • HY-162475
    Fluorofolin
    		Inhibitor 99.85%
    Fluorofolin is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.5 nM. Fluorofolin exhibits significant activity against P. aeruginosa.
    Fluorofolin
  • 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-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-169790
    Phomarin
    		Inhibitor 98.53%
    Phomarin is an inhibitor for dihydrofolate reductase (DHFR). Phomarin exhibits activity against Plasmodium parasites and fungi including Mycrobotryum violaceum and Botrytis cinerea. Phomarin can be used for the research of malaria and fungal infections.
    Phomarin
  • 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-137129
    10-Formyl-7,8-dihydrofolic acid
    		Substrate
    10-Formyl-7,8-dihydrofolic acid is a biologically active folic acid and growth promoter. 10-Formyl-7,8-dihydrofolic acid serves as a substrate for aminoimidazolecarboxamide ribonucleotide transformylase and dihydrofolate reductase (DHFR) to support catalytic reactions (with detection wavelengths of 552 nm and 340 nm, respectively). 10-Formyl-7,8-dihydrofolic acid not only promotes the growth of leukemia cells, but also effectively reverses the growth inhibition induced by antifolate drugs under folate-deficient conditions. 10-Formyl-7,8-dihydrofolic acid can be used in the research of leukemia.
    10-Formyl-7,8-dihydrofolic acid
  • HY-122045
    CB 3705
    		Inhibitor
    CB 3705 is a dihydrofolate reductase (DHFR) and thymidylate synthetase (TS) inhibitor. CB 3705 inhibits L1210 cells and mutant L1210 cell line (L1210:C15) with ID50s of 4.77 μM and 408 μM, respectively.
    CB 3705
Cat. No. Product Name / Synonyms Application Reactivity