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DHFR Inhibitors

" in MedChemExpress (MCE) Product Catalog:

54

Inhibitors & Agonists

1

Natural
Products

6

Isotope-Labeled Compounds

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas
  • HY-W003561
    DHFR-IN-3

    		Antifolate Parasite Infection
    DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor with the IC50 values of 19 μM and 12 μM in rat liver and P. carinii DHFR, respectively.
  • HY-137439
    Fanotaprim

    VYR-006

    		 Antifolate Infection
    Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis.
  • HY-153007
    DHFR-IN-5

    		Dihydrofolate reductase (DHFR) Infection
    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-156412
    DHFR-IN-10

    		Bacterial Infection
    DHFR-IN-10 (compound 4c) is a potent DHFR inhibitor, with an IC50 of 4.21 μM for M. tuberculosis DHFR enzyme. DHFR-IN-10 exhibits potent antituberculosis efficiency.
  • HY-156414
    DHFR-IN-11

    		Dihydrofolate reductase (DHFR) Infection
    DHFR-IN-11 (compound 6b) is inhibitor of DHFR, and has inhibitory potency versus M. tuberculosis DHFR enzyme with IC50 values 5.70 μM.
  • HY-B1902
    Diaveridine

    EGIS-5645

    		 Antifolate Bacterial Infection
    Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
  • HY-151159
    DHFR-IN-4

    		Dihydrofolate reductase (DHFR) EGFR Cancer
    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-143236
    DHFR-IN-1

    		Bacterial Fungal Infection
    DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249.
  • HY-W587663
    4′-DTMP

    		Dihydrofolate reductase (DHFR) Infection
    4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFR WT) and 34.3 nM (DHFR L28R), 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-143408
    OYYF-175

    		Bacterial Infection
    OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-
  • HY-156122
    DHFR-IN-8

    		Bacterial Dihydrofolate reductase (DHFR) Infection
    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-107033
    Tetroxoprim

    HE 781

    		 Antifolate Infection Inflammation/Immunology
    Tetroxoprim is an antimicrobial DHFR inhibitor.
  • HY-18062S
    Pyrimethamine-d3

    		Antifolate Parasite Infection
    Pyrimethamine-d3 is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR)[1][2].
  • HY-149633
    EGFR/HER2/DHFR-IN-3

    		EGFR Dihydrofolate reductase (DHFR) Apoptosis Cancer
    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-147661
    DHFR-IN-2

    		Antifolate Infection
    DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research.
  • HY-151459
    VEGFR-2/DHFR-IN-2

    		VEGFR Bacterial Dihydrofolate reductase (DHFR) Fungal Cancer Infection
    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-10373
    Trimetrexate

    CI-898

    		 Dihydrofolate reductase (DHFR) Antibiotic Antifolate Parasite Bacterial DNA/RNA Synthesis Infection Cancer
    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-10373A
    Trimetrexate trihydrochloride

    CI-898 trihydrochloride

    		 Dihydrofolate reductase (DHFR) Antibiotic Antifolate Parasite Bacterial DNA/RNA Synthesis Infection
    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-139743
    Aditoprime

    Aditoprim

    		 Antifolate Bacterial Infection
    Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics.
  • HY-151154
    EGFR/HER2/DHFR-IN-1

    		EGFR Cancer
    EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis.
  • HY-149200
    Lysine-methotrexate

    		Antifolate Inflammation/Immunology
    Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor.
  • HY-156123
    DHFR-IN-9

    		Bacterial Dihydrofolate reductase (DHFR) Cancer Infection
    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-10373B
    Trimetrexate isethionate

    CI-898 isethionate

    		 Dihydrofolate reductase (DHFR) Antibiotic Antifolate Parasite Bacterial DNA/RNA Synthesis Cancer Infection
    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-151458
    VEGFR-2/DHFR-IN-1

    		VEGFR Bacterial Dihydrofolate reductase (DHFR) Fungal Cancer Infection
    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-149699
    DHFR-IN-12

    		Dihydrofolate reductase (DHFR) Infection
    DHFR-IN-12 (Compound 5c) is a DHFR inhibitor which has good antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa in vitro, and can effectively reduce rat keratitis infection in vivo activity.
  • HY-156859
    NSC309401 dihydrochloride

    		Bacterial Inflammation/Immunology
    NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM).
  • HY-156859A
    NSC309401

    		Bacterial Infection
    NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM).
  • HY-117791
    (R)-Pralatrexate

    		Others Cancer
    (R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor.
  • HY-154807
    DQn-1

    		Bacterial Infection
    DQn-1 is a potent antifolate with activity against Mycobacterium tuberculosis (Mtb) (MIC90=0.03 µM). DQn-1 directly inhibits DHFR enzyme activity, with IC50s of 8.7 and 7.6 nM for Mtb and human DHFR enzyme, respectively.
  • HY-149632
    EGFR/HER2/DHFR-IN-2

    		Dihydrofolate reductase (DHFR) EGFR Cancer
    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-B0806
    Proguanil

    		Parasite Antifolate Infection
    Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
  • HY-B0806A
    Proguanil hydrochloride

    		Parasite Antifolate Infection
    Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
  • HY-10824B
    Talotrexin ammonium

    PT523 ammonium

    		 Others Cancer
    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.
  • HY-B0806AS
    Proguanil-d4 hydrochloride

    		Isotope-Labeled Compounds Parasite Antifolate Infection
    Proguanil-d4 (hydrochloride) is the deuterium labeled Proguanil hydrochloride. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor[1][2].
  • HY-B0806S1
    Proguanil-d4

    		Antifolate Parasite Infection
    Proguanil-d4 is the deuterium labeled Proguanil[1]. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor[2][3].
  • HY-10820B
    Pemetrexed disodium heptahydrate
    Maximum Cited Publications
    17 Publications Verification

    LY231514 disodium heptahydrate

    		 Antifolate Autophagy Cancer
    Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-13781
    Pemetrexed disodium hemipenta hydrate
    Maximum Cited Publications
    17 Publications Verification

    LY231514 disodium hemipenta hydrate

    		 Antifolate Autophagy Apoptosis Cancer
    Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-N10791
    Neobritannilactone B

    		Others Infection
    Neobritannilactone B, a sesquiterpene, can be isolated from the chloroform fraction of the I. britannica. Neobritannilactone B is cytotoxic. Other extracts of I. britannica are also Dihydrofolate reductase (DHFR) inhibitors, which inhibit Shigella dysenteriae type 1.
  • HY-B0806AS1
    Proguanil-d6 hydrochloride

    		Isotope-Labeled Compounds Parasite Antifolate Infection
    Proguanil-d6 hydrochloride is the deuterium labeled Proguanil hydrochloride (HY-B0806A). Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
  • HY-151158
    EGFR/HER2-IN-7

    		EGFR Cancer
    EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM).
  • HY-19095
    TNP-351

    		Antifolate Cancer
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
  • HY-151156
    EGFR/HER2-IN-6

    		EGFR Apoptosis Cancer
    EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
  • HY-151161
    EGFR/HER2-IN-8

    		EGFR Cancer
    EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
  • HY-10820
    Pemetrexed
    Maximum Cited Publications
    17 Publications Verification

    LY231514

    		 Antifolate Autophagy Cancer
    Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-18062
    Pyrimethamine
    5 Publications Verification

    Pirimecidan; Pirimetamin; RP 4753

    		 Antifolate Parasite Infection
    Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate.
  • HY-10820A
    Pemetrexed disodium
    Maximum Cited Publications
    17 Publications Verification

    LY231514 disodium

    		 Antifolate Autophagy Apoptosis Cancer
    Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-10824
    Talotrexin

    PT523

    		 Antifolate Dihydrofolate reductase (DHFR) Cancer
    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.
  • HY-122289
    Metioprim

    		Dihydrofolate reductase (DHFR) Bacterial Infection
    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-116387A
    WR99210 hydrochloride

    BRL 6231

    		 Dihydrofolate reductase (DHFR) Parasite Infection
    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-10820S
    Pemetrexed-d5

    LY231514-d5

    		 Antifolate Autophagy Cancer
    Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
  • HY-14518
    Aminopterin

    4-Aminofolic acid; APGA

    		 Antifolate Cancer Inflammation/Immunology
    Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.
  • HY-10820AS
    Pemetrexed-d5 disodium

    LY231514-dd5 (disodium)

    		 Antifolate Autophagy Apoptosis Cancer
    Pemetrexed-d5 (disodium) is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].
  • HY-116387
    WR99210
    2 Publications Verification

    BRL 6231 free base

    		 Dihydrofolate reductase (DHFR) Parasite Infection
    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-10446
    Pralatrexate
    3 Publications Verification

    		 Antifolate Apoptosis Cancer
    Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.