| S1210 |
Methotrexate
|
Methotrexate, 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. |
-
J Clin Invest, 2025, e190215
-
Theranostics, 2025, 15(10):4526-4549
-
Antimicrob Agents Chemother, 2025, e0047125.
|
|
| S1135 |
Pemetrexed disodium
|
Pemetrexed 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. |
-
Nat Commun, 2025, 16(1):8932
-
Cell Death Dis, 2024, 15(8):555
-
Cell Commun Signal, 2024, 22(1):375
|
|
| 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. |
-
iScience, 2024, 27(10):110862
-
Cell Rep, 2022, 38(9):110448
-
Front Pharmacol, 2022, 13:1032975
|
|
| S5971 |
Pemetrexed
|
Pemetrexed (LY231514) 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. |
-
Nat Commun, 2025, 16(1):7853
-
Nat Commun, 2025, 16(1):8476
-
Sci Adv, 2025, 11(4):eadp4765
|
|
| S5097 |
Methotrexate disodium
|
Methotrexate disodium, an 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. |
-
Chin Med J (Engl), 2023, 10.1097/CM9.0000000000002816
-
Pharmaceutics, 2023, 15(2)576
-
Pharmaceutics, 2023, 15(2)576
|
|
| S1497 |
Pralatrexate
|
Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis. |
-
Cell Rep Med, 2025, S2666-3791(25)00102-8
-
Br J Haematol, 2024, 10.1111/bjh.19658
-
Discov Oncol, 2024, 15(1):709
|
|
| S2006 |
Pyrimethamine
|
Pyrimethamine(RP 4753) is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug. |
-
Antimicrob Agents Chemother, 2025, e0047125.
-
Int J Parasitol Drugs Drug Resist, 2025, 29:100626
-
BMC Cancer, 2024, 24(1):116
|
|
| S1236 |
Leucovorin (Folinic acid) Calcium Pentahydrate
|
Leucovorin (Folinic acid) Calcium Pentahydrate is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.Solutions are unstable and should be fresh-prepared. |
-
J Exp Clin Cancer Res, 2025, 44(1):13
-
iScience, 2024, 27(10):110862
-
Cell Rep Med, 2023, 4(10):101200
|
|
| S2588 |
Calcium Folinate
|
Calcium Folinate is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy.Solutions are unstable and should be fresh-prepared. |
-
Drug Resist Updat, 2023, 71:101005
|
|
| S5790 |
Folinic acid (Leucovorin)
|
Folinic acid (Leucovorin) is a biological folic acid that increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase (TS).Solutions are unstable and should be fresh-prepared. |
-
Nat Cell Biol, 2024,
-
Nat Commun, 2022, 13(1):6308
|
|
| 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. |
-
Cell Rep, 2024, 43(7):114500
-
Sci Rep, 2024, 14(1):9167
-
Sci Rep, 2024, 14(1):9167
|
|
| S5264 |
L-5-Methyltetrahydrofolate calcium
|
Calcium L-5-methyltetrahydrofolate (L-5-MTHF-Ca) is a synthetic derivative of folic acid, the predominant, naturally occurring form of folate. |
|
|
| E4837 |
Trimethoprim (lactate)
|
Trimethoprim (lactate) is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), an essential enzyme responsible for the production of tetrahydrofolic acid (THF). By blocking this enzyme, trimethoprim prevents the synthesis of bacterial DNA, hindering bacterial survival. It is a standard antibiotic for treating urinary tract infections (UTIs). |
|
|
| S3082 |
Proguanil HCl(Atovaquone)
|
Proguanil hydrochloride(Chloroguanil, Chlorguanide hydrochloride), an antimalarial proagent acts as an inhibitor of dihydrofolate reductase (DHFR). Proguanil acts as a biguanide to enhance the Atovaquone effect. |
|
|
| A2491 |
Mirvetuximab (Anti-FOLR1)
|
Mirvetuximab (Anti-FOLR1) is a monoclonal antibody targeting FOLR1 (folate receptor 1). Mirvetuximab is the antibody moiety of novel folate receptor alpha (FRα)-targeting ADC (Mirvetuximab soravtansine). MW: 145.2 KD |
|
|
| A2492 |
Farletuzumab (Anti-FOLR1)
|
Farletuzumab (Anti-FOLR1) is a humanized monoclonal antibody with high affinity for FRα. It is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer. MW: 144.12 KD |
|
|
| E1003 |
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.
|
-
Mol Cancer Res, 2024, 22(1):82-93
|
|
| 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. |
|
|
| A2492 |
Farletuzumab (Anti-FOLR1)
|
Farletuzumab (Anti-FOLR1) is a humanized monoclonal antibody with high affinity for FRα. It is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer. MW: 144.12 KD |
|
|
| S1210 |
Methotrexate
|
Methotrexate, 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. |
- J Clin Invest, 2025, e190215
- Theranostics, 2025, 15(10):4526-4549
- Antimicrob Agents Chemother, 2025, e0047125.
|
|
| S1135 |
Pemetrexed disodium
|
Pemetrexed 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. |
- Nat Commun, 2025, 16(1):8932
- Cell Death Dis, 2024, 15(8):555
- Cell Commun Signal, 2024, 22(1):375
|
|
| 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. |
- iScience, 2024, 27(10):110862
- Cell Rep, 2022, 38(9):110448
- Front Pharmacol, 2022, 13:1032975
|
|
| S5971 |
Pemetrexed
|
Pemetrexed (LY231514) 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. |
- Nat Commun, 2025, 16(1):7853
- Nat Commun, 2025, 16(1):8476
- Sci Adv, 2025, 11(4):eadp4765
|
|
| S5097 |
Methotrexate disodium
|
Methotrexate disodium, an 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. |
- Chin Med J (Engl), 2023, 10.1097/CM9.0000000000002816
- Pharmaceutics, 2023, 15(2)576
- Pharmaceutics, 2023, 15(2)576
|
|
| S1497 |
Pralatrexate
|
Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis. |
- Cell Rep Med, 2025, S2666-3791(25)00102-8
- Br J Haematol, 2024, 10.1111/bjh.19658
- Discov Oncol, 2024, 15(1):709
|
|
| S2006 |
Pyrimethamine
|
Pyrimethamine(RP 4753) is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug. |
- Antimicrob Agents Chemother, 2025, e0047125.
- Int J Parasitol Drugs Drug Resist, 2025, 29:100626
- BMC Cancer, 2024, 24(1):116
|
|
| S2588 |
Calcium Folinate
|
Calcium Folinate is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy.Solutions are unstable and should be fresh-prepared. |
- Drug Resist Updat, 2023, 71:101005
|
|
| S5790 |
Folinic acid (Leucovorin)
|
Folinic acid (Leucovorin) is a biological folic acid that increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase (TS).Solutions are unstable and should be fresh-prepared. |
- Nat Cell Biol, 2024,
- Nat Commun, 2022, 13(1):6308
|
|
| E4837 |
Trimethoprim (lactate)
|
Trimethoprim (lactate) is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), an essential enzyme responsible for the production of tetrahydrofolic acid (THF). By blocking this enzyme, trimethoprim prevents the synthesis of bacterial DNA, hindering bacterial survival. It is a standard antibiotic for treating urinary tract infections (UTIs). |
|
|
| S3082 |
Proguanil HCl(Atovaquone)
|
Proguanil hydrochloride(Chloroguanil, Chlorguanide hydrochloride), an antimalarial proagent acts as an inhibitor of dihydrofolate reductase (DHFR). Proguanil acts as a biguanide to enhance the Atovaquone effect. |
|
|
| E1003 |
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.
|
- Mol Cancer Res, 2024, 22(1):82-93
|
|
| 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. |
|
|