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-178728
    BION106
    		Degrader
    BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites (Blue: Idasanutlin ligand (HY-15676); Pink: DHFR-TS ligand (HY-153007); Black: Linker (HY-W021401)).
    BION106
  • 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-173220
    DHFR-IN-23
    		Inhibitor
    DHFR-IN-23 (compound 5) is a dual DNA binders/DHFR inhibitor, with an IC50 of 0.08 μM for hDHFR. DHFR-IN-23 (compound 5) is also an apoptosis inducer. DHFR-IN-23 (compound 5) can be used for the research of ER+ breast cancer.
    DHFR-IN-23
  • 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-19885
    AR-102
    		Inhibitor
    AR-102 has inhibitory activity towards Staphylococcus aureus. AR-102 exhibits a competitive potent inhibition of the F98Y mutant DHFR (Ki = 0.22 nM). AR-102 has been determined as ternary complex with NADPH in both wild-type S. aureus DHFR and the TMP-resistant F98Y mutant enzyme.
    AR-102
  • 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-183053
    UCP1173
    		Inhibitor
    UCP1173, propargyl-linked antifolate, is an antibacterial agent. UCP1173 inhibits DHFR enzymes, with IC50 values of 0.014 μM for DfrB, 0.19 μM for DfrG, 0.27 μM for DfrA, and 0.091 μM for DfrK. UCP1173 inhibits growth of Staphylococcus aureus clinical isolates carrying dfrA, dfrG, or dfrK resistance genes. UCP1173 can be used for the research of bacterial infections.
    UCP1173
  • 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-182684
    MMV675968
    		Inhibitor
    MMV675968 is an inhibitor of Acinetobacter baumannii dihydrofolate reductase (AbDHFR) with an IC50 of 8.5 nM, and it exhibits selectivity against human DHFR. MMV675968 inhibits dihydrofolate reductase in Cryptosporidium, Plasmodium, and Escherichia coli, disrupting the thymidylate cycle and folate biosynthesis pathway. MMV675968 inhibits the growth of multiple A. baumannii strains, including clinical isolates and environmental isolates. MMV675968 is applicable to research related to A. baumannii infections.
    MMV675968
  • 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-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
  • HY-125647
    10-Deazaaminopterin
    		Inhibitor
    10-Deazaaminopterin is a potent inhibitor of dihydrofolate reductase. 10-Deazaaminopterin can used in study advanced cancer.
    10-Deazaaminopterin
  • HY-168069
    DHFR-IN-20
    		Inhibitor
    DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme.
    DHFR-IN-20
  • HY-179493
    DHFR-IN-25
    		Inhibitor
    DHFR-IN-25 (Compound N2) is a type of inhibitor of dihydrofolate reductase (DHFR). DHFR-IN-25 is a broad-spectrum and highly effective antibacterial agent, particularly showing significant effects on Candida albicans and Staphylococcus aureus. DHFR-IN-25 can be used for the study of local anti-infection.
    DHFR-IN-25
Cat. No. Product Name / Synonyms Application Reactivity