DHFR

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DHFR Signaling Pathway Map

DHFR Signaling Pathways

DHFR Products

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  • DHFR Inhibitors (13)
  • DHFR Modulators (1)
  • New DHFR Products
Catalog No. Product Name Information Product Use Citations Product Validations
E1003New Aminopterin Aminopterin (4-amino Folic Acid, 4-amino PGA, 4-Aminofolic acid, 4-Aminopteroylglutamic acid, Aminopteroylglutamic acid, APGA, NSC 739), a folic acid antagonist, is a competitive inhibitor of dihydrofolate reductase (DHFR) with Ki of 3.7 pM.
S1135 Pemetrexed (LY-231514) disodium Pemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S1210 Methotrexate (CL-14377) Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Nat Commun, 2021, 12(1):1676
Mol Syst Biol, 2021, 17(11):e10396
S1497 Pralatrexate (NSC 754230) Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.
J Clin Endocrinol Metab, 2021, dgab424
Biomol Ther (Seoul), 2021, 29(3):268-272
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2006 Pyrimethamine Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
PLoS Pathog, 2020, 16;16(3):e1008341
Front Microbiol, 2020, 11:616688
S2588 Calcium Levofolinate Calcium Levofolinate (Calcium Folinate, Levoleucovorin calcium, CL307782) is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy.
S3129 Trimethoprim Trimethoprim (BW 56-72, NIH 204, NSC-106568) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections.
S5097 Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
J Clin Med, 2021, 10(7)1431
Int J Mol Sci, 2021, 22(3)1194
S5136 Calcium folinate Calcium folinate (Leucovorin calcium, Folinic acid calcium salt, Wellcovorin) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives.
S5200 Diaveridine Diaveridine (AI3-23935, CCRIS-3784) is coccidiostat with anti-parasitic activity and also a dihydrofolate reductase (DHFR) inhibitor preventing folic acid synthesis in species of Pneumocystis.
S5927 Proguanil Proguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug. It inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication.
Sci Adv, 2021, 7(27)eabh3032
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
S0320 Cycloguanil hydrochloride Cycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes.
S0854 Metoprine Metoprine (BW 197U), a diaminopyrimidine derivative, is a potent inhibitor of histamine N-methyltransferase (HMT) that crosses the blood-brain barrier and increases brain histamine levels. Metoprine is an antifolate and antitumor agent.
S1236 Leucovorin (NSC -3590) Calcium Pentahydrate Leucovorin Calcium Pentahydrate (NSC -3590, Folinic acid) is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.
Adv Sci (Weinh), 2021, e2103360
Cell Prolif, 2021, e13031
Virus Res, 2021, 302:198469
E1003New Aminopterin Aminopterin (4-amino Folic Acid, 4-amino PGA, 4-Aminofolic acid, 4-Aminopteroylglutamic acid, Aminopteroylglutamic acid, APGA, NSC 739), a folic acid antagonist, is a competitive inhibitor of dihydrofolate reductase (DHFR) with Ki of 3.7 pM.
S1135 Pemetrexed (LY-231514) disodium Pemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S1210 Methotrexate (CL-14377) Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Nat Commun, 2021, 12(1):1676
Mol Syst Biol, 2021, 17(11):e10396
S1497 Pralatrexate (NSC 754230) Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.
J Clin Endocrinol Metab, 2021, dgab424
Biomol Ther (Seoul), 2021, 29(3):268-272
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2006 Pyrimethamine Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
PLoS Pathog, 2020, 16;16(3):e1008341
Front Microbiol, 2020, 11:616688
S2588 Calcium Levofolinate Calcium Levofolinate (Calcium Folinate, Levoleucovorin calcium, CL307782) is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy.
S3129 Trimethoprim Trimethoprim (BW 56-72, NIH 204, NSC-106568) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections.
S5097 Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
J Clin Med, 2021, 10(7)1431
Int J Mol Sci, 2021, 22(3)1194
S5136 Calcium folinate Calcium folinate (Leucovorin calcium, Folinic acid calcium salt, Wellcovorin) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives.
S5200 Diaveridine Diaveridine (AI3-23935, CCRIS-3784) is coccidiostat with anti-parasitic activity and also a dihydrofolate reductase (DHFR) inhibitor preventing folic acid synthesis in species of Pneumocystis.
S5927 Proguanil Proguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug. It inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication.
Sci Adv, 2021, 7(27)eabh3032
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
S0320 Cycloguanil hydrochloride Cycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes.
E1003New Aminopterin Aminopterin (4-amino Folic Acid, 4-amino PGA, 4-Aminofolic acid, 4-Aminopteroylglutamic acid, Aminopteroylglutamic acid, APGA, NSC 739), a folic acid antagonist, is a competitive inhibitor of dihydrofolate reductase (DHFR) with Ki of 3.7 pM.
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043