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antifolate agents

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antifolate (15) ADC Payload (6) Apoptosis (6) Bacterial (7) Dihydrofolate reductase (DHFR) (1) DNA/RNA Synthesis (7) Drug Metabolite (8) Fluorescent Dye (1) Histone Methyltransferase (2) Isotope-Labeled Compounds (5) Nucleoside Antimetabolite/Analog (1) Parasite (4) Reference Standards (3)
By Research Areas:	Cancer (18) Infection (6) Inflammation/Immunology (12) Metabolic Disease (4) Neurological Disease (3)

Inhibitors & Agonists

Fluorescent Dye

Isotope-Labeled Compounds

Targets Recommended: Antifolate

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14519

Methotrexate Maximum Cited Publications 76 Publications Verification Amethopterin; CL14377; WR19039	Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial	Infection Neurological Disease Inflammation/Immunology Cancer
Methotrexate (Amethopterin), an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-14519A

Methotrexate disodium Maximum Cited Publications 76 Publications Verification Amethopterin disodium; CL14377 disodium; WR19039 disodium	Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial	Inflammation/Immunology Cancer
Methotrexate (Amethopterin) disodium, an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-14519S

Methotrexate-d3	Antifolate DNA/RNA Synthesis ADC Payload Apoptosis	Inflammation/Immunology Cancer
Methotrexate-d₃ (Amethopterin-d₃) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-129441

Metoprine BW 197U	Histone Methyltransferase Antifolate	Neurological Disease Cancer
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT . Metoprine is an *antifolate* and antitumor agent .

HY-130569

7-Hydroxymethotrexate	Drug Metabolite	Inflammation/Immunology Cancer
7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-133887

Methotrexate α-tert-butyl ester	Antifolate DNA/RNA Synthesis	Cancer
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent .

HY-14519R

Methotrexate (Standard) Amethopterin (Standard); CL14377 (Standard); WR19039 (Standard)	Reference Standards Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial	Inflammation/Immunology Cancer
Methotrexate (Standard) is the analytical standard of Methotrexate. This product is intended for research and analytical applications. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-133624

1,1,3-Tribromoacetone 1 Publications Verification	Drug Metabolite	Cancer
1,1,3-Tribromoacetone is an impurity of Methotrexate (HY-14519) . Methotrexate, an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-175428

Antifolate agent 1	Antifolate	Cancer
Antifolate agent 1 is a 6-substituted pyrrolopyrimidine antifolate with a 1-carbon bridge. Antifolate agent 1 shows no activity against cells expressing FRα and FRβ, and has no GARFTase inhibitory activity. Antifolate agent 1 can be used as a negative control in the development of folate receptor-targeted antifolates .

HY-137773

N-Methyl pemetrexed	Drug Metabolite	Cancer
N-Methyl pemetrexed is an impurity of Pemetrexed. Pemetrexed is an antifolate cytotoxic agent that can be used for the research of cancer .

HY-151935

Antileishmanial agent-13	Parasite	Infection
Antileishmanial agent-13 is a quinoline-isatin hybrid, acts as an antileishmanial agent against L. Major Leishmania strain. Antileishmanial agent-13 acquires the antileishmanial activity via the anti-folate mechanism. Antileishmanial agent-13 has potent inhibition against both promastigote and amastigote forms with IC₅₀s of 0.604 μM and 0.508 μM, respectively .

HY-121151

(±)-Methotrexate (±)-Amethopterin; (±)-CL14377; (±)-WR19039	Antifolate	Others
(±)-Methotrexate ((±)-Amethopterin) is a racemate of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of Folic acid into Tetrahydrofolate, and inhibiting DNA synthesis .

HY-14519D

Methotrexate monohydrate Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate	Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial	Inflammation/Immunology Cancer
Methotrexate (Amethopterin) monohydrate, an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-14519AR

Methotrexate disodium (Standard) Amethopterin disodium (Standard); CL14377 disodium (Standard); WR19039 disodium (Standard)	Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial Reference Standards	Inflammation/Immunology Cancer
Methotrexate (disodium) (Standard) is the analytical standard of Methotrexate (disodium). This product is intended for research and analytical applications. Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-P2938

Glutamate carboxypeptidase Carboxypeptidase G	Antifolate	Cancer
Glutamate carboxypeptidase is an endo/exopeptidase targeting *folate* and antifolate agents. Glutamate carboxypeptidase regulates intracellular folate homeostasis by hydrolyzing γ-polyglutamate chains. Glutamate carboxypeptidase is promising for research of antifolate agents and cancers .

HY-121207

Denopterin Pteroylglutamic acid	Antifolate Nucleoside Antimetabolite/Analog	Cancer
Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an *antifolate* agent. Denopterin is an antimetabolite that has toxic effects on cells and can be used for cancer .

HY-155845

Antileishmanial agent-21	Parasite	Infection
Antileishmanial agent-21 (compound 4e) is an antileishmanial agent that targets the Leishmania pteridine reductase 1 (Lm-PTR1). Antileishmanial agent-21 has an anti-folate mechanism, and folic acid and leucovorin can reverse the anti-leishmanial activity of Antileishmanial agent-21. Antileishmanial agent-21 inhibits the Chloroquine (HY-17589A)-resistant strain of Plasmodium falciparum (RKL9) with an IC₅₀ of 0.0198-0.096 μM .

HY-14519S1

Methotrexate-d3 diammonium	Isotope-Labeled Compounds	Metabolic Disease Inflammation/Immunology Cancer
Methotrexate-d₃ diammonium is the deuterium labeled Methotrexate diammonium. Methotrexate (Amethopterin), an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-130569S1

7-Hydroxymethotrexate-d3	Isotope-Labeled Compounds Drug Metabolite	Metabolic Disease
7-Hydroxymethotrexate-d₃ is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-130569S

7-Hydroxymethotrexate-d3 sodium	Isotope-Labeled Compounds Drug Metabolite	Inflammation/Immunology Cancer
7-Hydroxymethotrexate-d₃ (sodium) is deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-130569S2

7-Hydroxymethotrexate-d3 ammonium	Isotope-Labeled Compounds Drug Metabolite	Metabolic Disease
7-Hydroxymethotrexate-d₃ (ammonium) is the deuterium labeled 7-Hydroxymethotrexate ammonium. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-155846

Antileishmanial agent-22	Parasite Bacterial	Infection
Antileishmanial agent-22 (compound 15b) is a parasite inhibitor and an antibacterial agent, with antileishmanial, antimalarial, and anti-tubercular activities. Antileishmanial agent-22 inhibits leishmanial (IC₅₀=0.408 μM) based on antifolate mechanism. And, Antileishmanial agent-22 inhibits Folic acid and Folinic acid at 100 μM with inhibitory rates of 88% and 94%, respectively. Antileishmanial agent-22 inhibits P. berghei in vivo and in vitro, with 96.67% suppression under 48.4 μM/kg/day and 0.038 μM (IC₅₀), respectively. Moreover, Antileishmanial agent-22 inhibits M. tuberculosis with MIC of 28.44 μM .

HY-W654227

7-Hydroxy methotrexate-d3 ammonium salt	Isotope-Labeled Compounds Drug Metabolite	Inflammation/Immunology
7-Hydroxy methotrexate-d₃ (ammonium salt) is deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-129441R

Metoprine (Standard) BW 197U (Standard)	Histone Methyltransferase Antifolate Reference Standards	Neurological Disease Cancer
Metoprine (Standard) is the analytical standard of Metoprine. This product is intended for research and analytical applications. Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT . Metoprine is an antifolate and antitumor agent .

HY-19242

MX-68	Antifolate	Inflammation/Immunology
MX-68 is an orally active antifolate agent. MX-68 can prolong the lifespan of MRL/lpr mice, delay the onset of proteinuria, and inhibit the elevation of serum blood urea nitrogen and cholesterol levels. MX-68 is also an anti-rheumatic agent, which exerts potent antiproliferative effects on rheumatoid arthritis-related cells and can inhibit arthritis in rats. MX-68 can be used in the research of autoimmune diseases such as autoimmune kidney disease and rheumatoid arthritis .

HY-D2435

MTX-PEG-Cy3	Fluorescent Dye	Inflammation/Immunology Cancer
CDDP-PEG-Cy3 is a MTX-PEG conjugate labeled with Cy3 (HY-D0822). The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. The maximum emission wavelength of Cy3 is approximately 562-570 nm. Methotrexate (Amethopterin; MTX) (HY-14519), an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-130569A

7-Hydroxymethotrexate sodium	Drug Metabolite	Metabolic Disease
7-Hydroxymethotrexate sodium is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-183053

UCP1173	Bacterial Dihydrofolate reductase (DHFR) Antifolate	Infection
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 .

HY-180373

WR 30090	Parasite	Infection
WR 30090 (Compound 37) is a broad-spectrum antimalarial agent that does not rely on the classical antifolate pathway. WR 30090 exhibits strong activity against a variety of chloroquine-sensitive and resistant Plasmodium falciparum strains, especially the highly resistant Vietnamese strain. WR 30090 shows high activity in mouse malaria tests, with a minimum effective dose of 5 mg/kg and a minimum cure dose of 20 mg/kg. WR 30090 can be used for research on acute malaria .

Cat. No.	Product Name	Type

HY-D2435

MTX-PEG-Cy3	Fluorescent Dye
CDDP-PEG-Cy3 is a MTX-PEG conjugate labeled with Cy3 (HY-D0822). The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. The maximum emission wavelength of Cy3 is approximately 562-570 nm. Methotrexate (Amethopterin; MTX) (HY-14519), an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

MTX-PEG-Cy3

Fluorescent Dye

CDDP-PEG-Cy3 is a MTX-PEG conjugate labeled with Cy3 (HY-D0822). The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. The maximum emission wavelength of Cy3 is approximately 562-570 nm. Methotrexate (Amethopterin; MTX) (HY-14519), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

Cat. No.	Product Name	Chemical Structure

HY-14519S

Methotrexate-d3
Methotrexate-d₃ (Amethopterin-d₃) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

Methotrexate-d3

Methotrexate-d₃ (Amethopterin-d₃) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-14519S1

Methotrexate-d3 diammonium
Methotrexate-d₃ diammonium is the deuterium labeled Methotrexate diammonium. Methotrexate (Amethopterin), an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

Methotrexate-d3 diammonium

Methotrexate-d₃ diammonium is the deuterium labeled Methotrexate diammonium. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .

HY-130569S1

7-Hydroxymethotrexate-d3
7-Hydroxymethotrexate-d₃ is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-130569S

7-Hydroxymethotrexate-d3 sodium
7-Hydroxymethotrexate-d₃ (sodium) is deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-130569S2

7-Hydroxymethotrexate-d3 ammonium
7-Hydroxymethotrexate-d₃ (ammonium) is the deuterium labeled 7-Hydroxymethotrexate ammonium. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

HY-W654227

7-Hydroxy methotrexate-d3 ammonium salt
7-Hydroxy methotrexate-d₃ (ammonium salt) is deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .

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