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Results for "

antifolate

" in MedChemExpress (MCE) Product Catalog:

39

Inhibitors & Agonists

7

Isotope-Labeled Compounds

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    (R)-Pralatrexate
  • HY-149459A
    Phototrexate

    (E)-azoMTX

    		 Dihydrofolate reductase (DHFR) Cancer
    Phototrexate is a photoswitchable inhibitor of the human dihydrofolate reductase (DHFR). Phototrexate has antifolate and antiproliferative properties, which can be used for the research of cancer .
    Phototrexate
  • HY-137267
    10-Methyl-10-deazaaminopterin

    		Antifolate Cancer
    10-Methyl-10-deazaaminopterin is a folate analog and an antifolate. 10-Methyl-10-deazaaminopterin can be used for the research of cancer .
    10-Methyl-10-deazaaminopterin
  • 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 .
    Talotrexin ammonium
  • 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-
    OYYF-175
  • 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 .
    TNP-351
  • HY-130569
    7-Hydroxymethotrexate

    		Drug Metabolite Inflammation/Immunology Cancer
    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 .
    7-Hydroxymethotrexate
  • 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 .
    Talotrexin
  • HY-10446
    Pralatrexate
    4 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.
    Pralatrexate
  • HY-14521
    Lometrexol
    1 Publications Verification

    DDATHF

    		 Antifolate Apoptosis Caspase Bcl-2 Family Cancer
    Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
    Lometrexol
  • HY-14521B
    Lometrexol hydrate
    1 Publications Verification

    DDATHF hydrate

    		 Antifolate Apoptosis Caspase Bcl-2 Family Cancer
    Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
    Lometrexol hydrate
  • HY-14521A
    Lometrexol disodium
    1 Publications Verification

    DDATHF disodium

    		 Antifolate Apoptosis Caspase Bcl-2 Family Cancer
    Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
    Lometrexol disodium
  • 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 .
    N-Methyl pemetrexed
  • HY-14523
    LY 254155

    		Antifolate Cancer
    LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
    LY 254155
  • HY-105934A
    Ketotrexate sodium

    Emofolin sodium; 5-methyltetrahydrohomofolate sodium; NSC 139490 sodium

    		 Antifolate Inflammation/Immunology Cancer
    Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases .
    Ketotrexate sodium
  • HY-13781
    Pemetrexed disodium hemipenta hydrate
    15+ Cited Publications

    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.
    Pemetrexed disodium hemipenta hydrate
  • HY-10820B
    Pemetrexed disodium heptahydrate
    15+ Cited Publications

    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.
    Pemetrexed disodium heptahydrate
  • HY-10820
    Pemetrexed
    15+ Cited Publications

    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 .
    Pemetrexed
  • HY-10820A
    Pemetrexed disodium
    15+ Cited Publications

    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 .
    Pemetrexed disodium
  • 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 .
    Methotrexate α-tert-butyl ester
  • HY-133624
    1,1,3-Tribromoacetone

    		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 .
    1,1,3-Tribromoacetone
  • HY-107981
    LSN 3213128
    1 Publications Verification

    		 Antifolate Cancer
    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity .
    LSN 3213128
  • 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 .
    Metoprine
  • HY-14519
    Methotrexate
    Maximum Cited Publications
    30 Publications Verification

    Amethopterin; CL14377; WR19039

    		 Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis Bacterial 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) .
    Methotrexate
  • HY-14519D
    Methotrexate monohydrate

    Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate

    		 Antifolate DNA/RNA Synthesis ADC Cytotoxin 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) .
    Methotrexate monohydrate
  • HY-14519A
    Methotrexate disodium
    Maximum Cited Publications
    30 Publications Verification

    Amethopterin disodium; CL14377 disodium; WR19039 disodium
    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) .
    Methotrexate disodium
  • 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].
    Pemetrexed-d5
  • HY-10820AS
    Pemetrexed-d5 disodium

    LY231514-dd5 disodium

    		 Isotope-Labeled Compounds 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].
    Pemetrexed-d5 disodium
  • 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 .
    DQn-1
  • 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 (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[1][2].
    7-Hydroxymethotrexate-d3 sodium
  • HY-130569S1
    7-Hydroxymethotrexate-d3

    		Drug Metabolite Metabolic Disease
    7-Hydroxymethotrexate-d3 is the 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[1][2].
    7-Hydroxymethotrexate-d3
  • HY-130569S2
    7-Hydroxymethotrexate-d3 ammonium

    		Drug Metabolite Metabolic Disease
    7-Hydroxymethotrexate-d3 (ammonium) is the deuterium labeled 7-Hydroxymethotrexate ammonium. 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[1][2].
    7-Hydroxymethotrexate-d3 ammonium
  • 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) .
    Methotrexate-d3 diammonium
  • HY-13617
    Edatrexate

    CGP 30694

    		 Antifolate Cancer
    Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck .
    Edatrexate
  • HY-14519S
    Methotrexate-d3

    		Antifolate DNA/RNA Synthesis ADC Cytotoxin 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)[1][2][3].
    Methotrexate-d3
  • 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 .
    Antileishmanial agent-13
  • HY-108251
    Methotrexate metabolite
    1 Publications Verification

    DAMPA

    		 Antifolate Drug Metabolite Dihydrofolate reductase (DHFR) Parasite Infection Inflammation/Immunology
    Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent . Methotrexate metabolite is an antimalarial agent, which inhibits the parasite growth with an IC50 of 446 nM against the antifolate-sensitive strain and 812 nM against the highly resistant strain under physiological folate conditions. Methotrexate metabolite is inactive against mammalian cells. Methotrexate metabolite is a minimal inhibitor of dihydrofolate reductase among metabolites of methotrexate .
    Methotrexate metabolite
  • 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 .
    Antileishmanial agent-21
  • 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 .
    Antileishmanial agent-22

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