Search Result
Results for "
antifolate
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-117791
-
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Others
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Cancer
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(R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor .
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-
-
- HY-149459A
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(E)-azoMTX
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Dihydrofolate reductase (DHFR)
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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 .
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-
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- HY-137267
-
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Antifolate
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Cancer
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10-Methyl-10-deazaaminopterin is a folate analog and an antifolate. 10-Methyl-10-deazaaminopterin can be used for the research of cancer .
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-
-
- HY-10824B
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PT523 ammonium
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Others
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Cancer
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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 .
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-
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- HY-143408
-
|
Bacterial
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Infection
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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-
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-
-
- HY-19095
-
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Antifolate
|
Cancer
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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 .
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-
-
- HY-130569
-
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Drug Metabolite
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Inflammation/Immunology
Cancer
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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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-
-
- HY-10824
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PT523
|
Antifolate
Dihydrofolate reductase (DHFR)
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Cancer
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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 .
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-
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- HY-10446
-
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Antifolate
Apoptosis
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Cancer
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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.
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-
-
- HY-14521
-
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 .
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-
-
- HY-14521B
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DDATHF hydrate
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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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 .
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-
-
- HY-14521A
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DDATHF disodium
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Antifolate
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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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 .
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-
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- HY-137773
-
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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 .
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-
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- HY-14523
-
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Antifolate
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Cancer
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LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
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-
-
- HY-105934A
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Emofolin sodium; 5-methyltetrahydrohomofolate sodium; NSC 139490 sodium
|
Antifolate
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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 .
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-
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- HY-13781
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LY231514 disodium hemipenta hydrate
|
Antifolate
Autophagy
Apoptosis
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Cancer
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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.
|
-
-
- HY-10820B
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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.
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-
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- HY-10820
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LY231514
|
Antifolate
Autophagy
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Cancer
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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 .
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-
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- HY-10820A
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LY231514 disodium
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Antifolate
Autophagy
Apoptosis
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Cancer
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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 .
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-
-
- HY-133887
-
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Antifolate
DNA/RNA Synthesis
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Cancer
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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 .
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-
-
- HY-133624
-
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Drug Metabolite
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Cancer
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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 .
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-
-
- HY-107981
-
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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 .
|
-
-
- HY-129441
-
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 .
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-
-
- HY-14519
-
Methotrexate
Maximum Cited Publications
32 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) .
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-
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- HY-14519D
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Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
Bacterial
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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-14519A
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Amethopterin disodium; CL14377 disodium; WR19039 disodium
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
Bacterial
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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) .
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-
-
- HY-10820S
-
LY231514-d5
|
Antifolate
Autophagy
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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].
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-
-
- HY-10820AS
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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].
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-
-
- HY-154807
-
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Bacterial
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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 .
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-
-
- HY-130569S
-
|
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].
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-
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- HY-130569S1
-
|
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].
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-
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- HY-130569S2
-
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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].
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-
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- HY-14519S1
-
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Isotope-Labeled Compounds
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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) .
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-
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- HY-13617
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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 .
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-
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- HY-14519S
-
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Inflammation/Immunology
Cancer
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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].
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-
-
- HY-151935
-
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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 .
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-
-
- HY-108251
-
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 .
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-
-
- HY-155845
-
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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-155846
-
|
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 .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10820S
-
|
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].
|
-
-
- HY-10820AS
-
|
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].
|
-
-
- HY-130569S
-
|
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].
|
-
-
- HY-130569S1
-
|
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].
|
-
-
- HY-130569S2
-
|
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].
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-
-
- HY-14519S1
-
|
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-14519S
-
|
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].
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-
Cat. No. |
Product Name |
|
Classification |
-
- HY-10446
-
|
|
Alkynes
|
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.
|
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