DHFR

Signaling Pathway Map

Research Area

Inhibitory Selectivity

DHFR Products

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

S2006

Pyrimethamine

Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.

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.

S2588New

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.

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.

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.

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.

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.

S0320

Cycloguanil hydrochloride

Cycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

S2006

Pyrimethamine

Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.

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.

S2588New

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.

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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S0320

Cycloguanil hydrochloride

Cycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes.

Catalog No. Information Product Use Citations Product Validations
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.

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.