Search Result
Results for "
dihydrofolate reductase (DHFR) inhibitor
" in MedChemExpress (MCE) Product Catalog:
14
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-10820
-
Pemetrexed
Maximum Cited Publications
39 Publications Verification
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 .
|
-
-
- HY-18062
-
|
Pirimecidan; Pirimetamin; RP 4753
|
Antifolate
Parasite
|
Infection
Cancer
|
|
Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate .
|
-
-
- HY-10820A
-
|
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 .
|
-
-
- HY-10446
-
|
|
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.
|
-
-
- HY-10373
-
|
CI-898
|
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
|
-
-
- HY-I0447
-
|
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
4-Aminosalicylic acid is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. 4-Aminosalicylic acid exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). 4-Aminosalicylic acid is orally active .
|
-
-
- HY-13781
-
-
-
- HY-14518
-
|
4-Aminofolic acid; APGA
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
-
- HY-10820B
-
|
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.
|
-
-
- HY-B0806
-
|
|
Parasite
Antifolate
|
Infection
|
|
Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .
|
-
-
- HY-116387
-
WR99210
4 Publications Verification
BRL 6231 free base
|
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine< (HY-18062)-resistant P. falciparum strains) as well as T. gondii .
|
-
-
- HY-153007
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity .
|
-
-
- HY-B0806A
-
|
|
Parasite
Antifolate
|
Infection
|
|
Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
|
-
-
- HY-12784A
-
|
Chlorguanide triazine hydrochloride
|
Antifolate
Parasite
DNA/RNA Synthesis
STAT
|
Infection
Cancer
|
|
Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
-
- HY-10820R
-
|
LY231514 (Standard)
|
Reference Standards
Antifolate
Autophagy
|
Cancer
|
|
Pemetrexed (Standard) is the analytical standard of Pemetrexed. This product is intended for research and analytical applications. 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 .
|
-
-
- HY-I0447A
-
|
4-Aminosalicylic acid sodium salt dihydrate
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
Sodium 4-aminosalicylate dihydrate (4-Aminosalicylic acid sodium salt dihydrate) is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. Sodium 4-aminosalicylate dihydrate exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). Sodium 4-aminosalicylate dihydrate is orally active .
|
-
-
- HY-B1902
-
|
EGIS-5645
|
Antifolate
Bacterial
|
Infection
|
|
Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
|
-
-
- HY-162475
-
-
-
- HY-169790
-
|
|
Dihydrofolate reductase (DHFR)
Parasite
Fungal
|
Infection
|
|
Phomarin is an inhibitor for dihydrofolate reductase (DHFR). Phomarin exhibits activity against Plasmodium parasites and fungi including Mycrobotryum violaceum and Botrytis cinerea. Phomarin can be used for the research of malaria and fungal infections .
|
-
-
- HY-W003561
-
|
|
Antifolate
Parasite
|
Infection
|
|
DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor with the IC50 values of 19 μM and 12 μM in rat liver and P. carinii DHFR, respectively .
|
-
-
- HY-106434
-
|
BW 301U; NSC 351521
|
Dihydrofolate reductase (DHFR)
|
Infection
Cancer
|
|
Piritrexim (BW 301U) is a potent dihydrofolate reductase (DHFR) inhibitor against Pneumocystis carinii and Toxoplasma gondii, with IC50 values of 0.038 and 0.011 μM, respectively. Piritrexim can be used for acquired immune deficiency syndrome (AIDS) research. Piritrexim also is an anticancer agent .
|
-
-
- HY-116387A
-
|
BRL 6231
|
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii .
|
-
-
- HY-151159
-
|
|
Dihydrofolate reductase (DHFR)
EGFR
|
Cancer
|
|
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells .
|
-
-
- HY-179415
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
|
DHFR-IN-24, a benzothiazole derivative, is a dihydrofolate reductase (DHFR) inhibitor. DHFR-IN-24 has intrinsic antibacterial activity against both Gram-positive and Gram-negative strains. DHFR-IN-24 synergistically combines DHFR inhibition with photodynamic therapy (PDT) for enhanced antibacterial activity against multidrug-resistant pathogens .
|
-
-
- HY-18062R
-
|
Pirimecidan (Standard); Pirimetamin (Standard); RP 4753 (Standard)
|
Reference Standards
Antifolate
Parasite
|
Infection
|
|
Pyrimethamine (Standard) is the analytical standard of Pyrimethamine. This product is intended for research and analytical applications. Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate .
|
-
-
- HY-149200
-
-
-
- HY-12784
-
|
Chlorguanide triazine
|
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
Cancer
|
|
Cycloguanil (Chlorguanide triazine) is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
-
- HY-160254
-
-
-
- HY-116039
-
|
Ro11-8958
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
|
Epiroprim (Ro11-8958) is a selective dihydrofolate reductase (DHFR) inhibitor. Epiroprim displays excellent activity against staphylococci, enterococci, pneumococci, and streptococci .
|
-
-
- HY-139743
-
|
Aditoprim
|
Antifolate
Bacterial
|
Infection
|
|
Aditoprime (Aditoprim) is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR, respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics .
|
-
-
- HY-12784AR
-
|
Chlorguanide triazine hydrochloride (Standard)
|
Reference Standards
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
Cancer
|
|
Cycloguanil hydrochloride (Standard) is the analytical standard of Cycloguanil hydrochloride (HY-12784A). This product is intended for research and analytical applications. Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
-
- HY-18062S
-
|
|
Isotope-Labeled Compounds
Antifolate
Parasite
|
Infection
|
|
Pyrimethamine-d3 is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR) .
|
-
-
- HY-10373A
-
|
CI-898 trihydrochloride
|
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Trimetrexate (CI-898) trihydrochloride is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
|
-
-
- HY-B0806S1
-
|
|
Antifolate
Parasite
|
Infection
|
|
Proguanil-d4 is the deuterium labeled Proguanil . Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .
|
-
-
- HY-19095
-
|
|
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 .
|
-
-
- HY-10373B
-
|
CI-898 isethionate
|
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
|
-
-
- HY-122289
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
|
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
|
-
-
- HY-10820BR
-
|
LY231514 disodium heptahydrate (Standard)
|
Reference Standards
Antifolate
Autophagy
|
Cancer
|
|
Pemetrexed (disodium heptahydrate) (Standard) is the analytical standard of Pemetrexed (disodium heptahydrate). This product is intended for research and analytical applications. 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.
|
-
-
- HY-169211
-
-
-
- HY-161064
-
|
|
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
DHFR-IN-15 (compound 34) is a dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity. DHFR-IN-15 effectively binds to DHFR in cells, reducing DHFR levels to 10 nM .
|
-
-
- HY-161063
-
-
-
- HY-153007A
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 hydrochloride is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 hydrochloride shows anti-malaria activity .
|
-
-
- HY-137439
-
|
VYR-006
|
Antifolate
|
Infection
|
|
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis .
|
-
-
- HY-161292
-
-
-
- HY-179493
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
Fungal
|
Infection
|
|
DHFR-IN-25 (Compound N2) is a type of inhibitor of dihydrofolate reductase (DHFR). DHFR-IN-25 is a broad-spectrum and highly effective antibacterial agent, particularly showing significant effects on Candida albicans and Staphylococcus aureus. DHFR-IN-25 can be used for the study of local anti-infection .
|
-
-
- HY-B1902R
-
|
EGIS-5645 (Standard)
|
Reference Standards
Antifolate
Bacterial
|
Infection
|
|
Diaveridine (Standard) is the analytical standard of Diaveridine. This product is intended for research and analytical applications. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
|
-
-
- HY-117791
-
|
|
Antifolate
|
Cancer
|
|
(R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor .
|
-
-
- HY-147661
-
|
|
Antifolate
|
Infection
|
|
DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research .
|
-
-
- HY-121207
-
|
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-156122
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
|
DHFR-IN-8 (compound 6r) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-8 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=15.6 ng/mL) in mouse models of systemic infection and thigh infection .
|
-
- HY-B1902S
-
|
EGIS-5645-d6
|
Isotope-Labeled Compounds
Antifolate
Bacterial
|
Infection
|
|
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
|
-
- HY-139743R
-
|
Aditoprim (Standard)
|
Reference Standards
Antifolate
Bacterial
|
Infection
|
|
Aditoprime (Standard) is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR, respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics .
|
-
- HY-118251
-
|
|
Antifolate
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
|
-
- HY-143408
-
|
|
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-spectrum antibacterial activities, especially against multi-drug resistant Gram-Negative-strains .
|
-
- HY-143236
-
|
|
Bacterial
Fungal
|
Infection
|
|
DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249 .
|
-
- HY-B0806AS
-
|
|
Isotope-Labeled Compounds
Parasite
Antifolate
|
Infection
|
|
Proguanil-d4 (hydrochloride) is the deuterium labeled Proguanil hydrochloride. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
|
-
- HY-177337
-
|
N-Didesmethyl-ADP
|
Drug Metabolite
Antifolate
Bacterial
|
Infection
|
|
N-Didesmethyladitoprim is a metabolite of Aditoprime (HY-139743). Aditoprime is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR , respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics .
|
-
- HY-12784S
-
|
Chlorguanide triazine-d6
|
Isotope-Labeled Compounds
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
Cancer
|
|
Cycloguanil-d6 (Chlorguanide triazine-d6) is the deuterium labeled Cycloguanil (HY-12784). Cycloguanil is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
- HY-12784AS
-
|
Chlorguanide triazine-d4 hydrochloride
|
Isotope-Labeled Compounds
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
Cancer
|
|
Cycloguanil-d4 (Chlorguanide triazine-d4) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
- HY-12784AS1
-
|
Chlorguanide triazine-d6 hydrochloride
|
Isotope-Labeled Compounds
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
|
|
Cycloguanil-d6 (Chlorguanide triazine-d6) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
- HY-115836
-
|
|
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
DDPO is an inhibitor for dihydrofolate reductase (DHFR) with an IC50 of 0.035 µM. DDPO inhibits the cell growth of cancer cell L1210 and WI-L2with IC50 of 5 and 0.28 µM .
|
-
- HY-12784S1
-
|
Chlorguanide triazine-d6 nitrate
|
Isotope-Labeled Compounds
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
Cancer
|
|
Cycloguanil-d6 (Chlorguanide triazine-d6) nitrate is the deuterium labeled Cycloguanil nitrate. Cycloguanil nitrate is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil nitrate blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil nitrate inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil nitrate also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
- HY-111202R
-
|
TSH-888 (Standard)
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Reference Standards
Cytochrome P450
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Inflammation/Immunology
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Proguanil (hydrochloride) (Standard) is the analytical standard of Proguanil (hydrochloride). This product is intended for research and analytical applications. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-B0806AR
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Reference Standards
Parasite
Antifolate
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Infection
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Proguanil (hydrochloride) (Standard) is the analytical standard of Proguanil (hydrochloride). This product is intended for research and analytical applications. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-B0806R
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Reference Standards
Parasite
Antifolate
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Infection
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Proguanil (Standard) is the analytical standard of Proguanil. This product is intended for research and analytical applications. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-159899
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Bacterial
Antibiotic
Dihydrofolate reductase (DHFR)
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DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase) inhibitor belonging to the class of 2,4-diaminopyrimidine compounds. DHFR-IN-22 exhibits significant inhibitory activity against purified DHFR enzyme and major species of nontuberculous mycobacteria (NTM), namely Mycobacterium avium and Mycobacterium abscessus. It shows an IC50 of 1.1 nM and MIC of 1.5 μg/mL against M. abscessus, and an IC50 of 6.3 nM and MIC of 0.1 μg/mL against M. avium. Additionally, it demonstrates an IC50 of 2100 nM against human DHFR. DHFR-IN-22 holds potential for studying novel strategies to combat NTM infections .
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- HY-N10791
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Others
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Infection
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Neobritannilactone B, a sesquiterpene, can be isolated from the chloroform fraction of the I. britannica. Neobritannilactone B is cytotoxic. Other extracts of I. britannica are also Dihydrofolate reductase (DHFR) inhibitors, which inhibit Shigella dysenteriae type 1 .
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- HY-168069
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Parasite
Dihydrofolate reductase (DHFR)
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Infection
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DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
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- HY-B0806AS1
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Isotope-Labeled Compounds
Parasite
Antifolate
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Infection
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Proguanil-d6 hydrochloride is the deuterium labeled Proguanil hydrochloride (HY-B0806A). Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-156123
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Dihydrofolate reductase (DHFR)
Bacterial
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Infection
Cancer
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DHFR-IN-9 (compound 8A) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-9 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=0.25 μg/mL) and has anti-infective effects in mouse models of systemic infection and thigh infection caused by it (dose: 2.5 mg /kg, 5 mg/kg; ip). DHFR-IN-9 has stronger anticancer activity than paclitaxel (Y-B0015) in a mouse model of breast cancer (dose: 2.5 mg/kg; ip; once every 3 days) .
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- HY-22252
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Antibiotic
Bacterial
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Infection
Inflammation/Immunology
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4-Aminosalicylic acid hemicalcium is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. 4-Aminosalicylic acid hemicalcium exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). 4-Aminosalicylic acid hemicalcium is orally active .
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- HY-10820S
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LY231514-d5
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Antifolate
Autophagy
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Cancer
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Pemetrexed-d5 is the deuterium labeled Pemetrexed . 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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- HY-122045
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- HY-10820AS
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LY231514-d5 disodium
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Isotope-Labeled Compounds
Antifolate
Autophagy
Apoptosis
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Cancer
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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 .
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- HY-168918
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Parasite
Dihydrofolate reductase (DHFR)
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Infection
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Insecticidal agent 19 (Compound 7b) exhibits antimalarial activity by inhibiting dihydrofolate
reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) through the folic acid metabolic pathway. Insecticidal agent 19 inhibits Leishmania major promastigote and amastigote with IC50 of 1.43 μM and 3.78 μM .
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- HY-13781R
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LY231514 disodium hemipenta hydrate (Standard)
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Antifolate
Autophagy
Apoptosis
Reference Standards
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Cancer
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Pemetrexed (disodium hemipenta hydrate) (Standard) is the analytical standard of Pemetrexed (disodium hemipenta hydrate). This product is intended for research and analytical applications. 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.
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- HY-I0447R
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Reference Standards
Antibiotic
Bacterial
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Infection
Inflammation/Immunology
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4-Aminosalicylic acid (Standard) is the analytical standard of 4-Aminosalicylic acid. This product is intended for research and analytical applications. 4-Aminosalicylic acid is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. 4-Aminosalicylic acid exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). 4-Aminosalicylic acid is orally active .
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- HY-14518R
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4-Aminofolic acid (Standard); APGA (Standard)
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Reference Standards
Antifolate
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Inflammation/Immunology
Cancer
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Aminopterin (Standard) is the analytical standard of Aminopterin. This product is intended for research and analytical applications. Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
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- HY-W769288
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LY231514 disodium-13C5
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Isotope-Labeled Compounds
Apoptosis
Antifolate
Autophagy
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Cancer
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Pemetrexed disodium- 13C5 (LY231514 disodium- 13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). 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-I0447AR
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4-Aminosalicylic acid sodium salt dihydrate (Standard)
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Reference Standards
Antibiotic
Bacterial
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Infection
Inflammation/Immunology
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Sodium 4-aminosalicylate (dihydrate) (Standard) is the analytical standard of Sodium 4-aminosalicylate (dihydrate). This product is intended for research and analytical applications. Sodium 4-aminosalicylate dihydrate (4-Aminosalicylic acid sodium salt dihydrate) is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. Sodium 4-aminosalicylate dihydrate exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). Sodium 4-aminosalicylate dihydrate is orally active .
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- HY-10446R
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Reference Standards
Antifolate
Apoptosis
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Cancer
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Pralatrexate (Standard) is the analytical standard of Pralatrexate. This product is intended for research and analytical applications. 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-105714
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Dihydrofolate reductase (DHFR)
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Endocrinology
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Etoprine is a potent orally active dihydrofolate reductase (DHFR) inhibitor. Etoprine competitively inhibits testicular DHFR to disrupt tetrahydrofolate and DNA synthesis in rapidly dividing cells. Etoprine acts as an antifertility agent in male mice and reduces fecundity in male rats .
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- HY-182684
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Bacterial
Dihydrofolate reductase (DHFR)
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Infection
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MMV675968 is an inhibitor of Acinetobacter baumannii dihydrofolate reductase (AbDHFR) with an IC50 of 8.5 nM, and it exhibits selectivity against human DHFR. MMV675968 inhibits dihydrofolate reductase in Cryptosporidium, Plasmodium, and Escherichia coli, disrupting the thymidylate cycle and folate biosynthesis pathway. MMV675968 inhibits the growth of multiple A. baumannii strains, including clinical isolates and environmental isolates. MMV675968 is applicable to research related to A. baumannii infections .
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- HY-181100
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Dihydrofolate reductase (DHFR)
Bacterial
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Infection
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DHFR-IN-26 is an Escherichia coli dihydrofolate reductase (ecDHFR) inhibitor with an IC50 of 0.75 nM. DHFR-IN-26 exerts broad-spectrum antibacterial activity. DHFR-IN-26 disrupts folate metabolism, nucleotide synthesis, and bacterial amino acid metabolic pathways. DHFR-IN-26 disrupts bacterial inner membranes, inhibited biofilm formation, and attenuated phage-related processes. DHFR-IN-26 shows lower toxicity to non-cancerous cells. DHFR-IN-26 can be used for the research of bacterial infections (including infections caused by methicillin-resistant Staphylococcus aureus, multidrug-resistant Escherichia coli, multidrug-resistant Pseudomonas aeruginosa, and lysogenic bacteria) .
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- HY-10373R
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CI-898 (Standard)
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Reference Standards
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
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Infection
Cancer
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Trimetrexate (Standard) is the analytical standard of Trimetrexate (HY-10373). This product is intended for research and analytical applications. Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
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- HY-I0447S
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Isotope-Labeled Compounds
Antibiotic
Bacterial
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Infection
Inflammation/Immunology
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4-Aminosalicylic acid-d6 is the deuterium labeled 4-Aminosalicylic acid (HY-I0447). 4-Aminosalicylic acid is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. 4-Aminosalicylic acid exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). 4-Aminosalicylic acid is orally active .
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- HY-10446S1
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Isotope-Labeled Compounds
Antifolate
Apoptosis
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Cancer
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Pralatrexate- 13C5, 15N is the 13C- and 15N-labeled Pralatrexate (HY-10446). 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-137357
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NSC 305986; γ-MBMTX
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Dihydrofolate reductase (DHFR)
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Cancer
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5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-18062S
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Pyrimethamine-d3 is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR) .
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- HY-B0806S1
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Proguanil-d4 is the deuterium labeled Proguanil . Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-B1902S
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Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
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- HY-B0806AS
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Proguanil-d4 (hydrochloride) is the deuterium labeled Proguanil hydrochloride. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-12784S
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1 Publications Verification
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Cycloguanil-d6 (Chlorguanide triazine-d6) is the deuterium labeled Cycloguanil (HY-12784). Cycloguanil is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
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- HY-12784AS
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Cycloguanil-d4 (Chlorguanide triazine-d4) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
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- HY-12784AS1
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Cycloguanil-d6 (Chlorguanide triazine-d6) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
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- HY-12784S1
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Cycloguanil-d6 (Chlorguanide triazine-d6) nitrate is the deuterium labeled Cycloguanil nitrate. Cycloguanil nitrate is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil nitrate blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil nitrate inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil nitrate also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
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- HY-B0806AS1
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Proguanil-d6 hydrochloride is the deuterium labeled Proguanil hydrochloride (HY-B0806A). Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
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- HY-10820S
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Pemetrexed-d5 is the deuterium labeled Pemetrexed . 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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- HY-10820AS
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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 .
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- HY-W769288
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Pemetrexed disodium- 13C5 (LY231514 disodium- 13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). 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-I0447S
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4-Aminosalicylic acid-d6 is the deuterium labeled 4-Aminosalicylic acid (HY-I0447). 4-Aminosalicylic acid is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. 4-Aminosalicylic acid exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). 4-Aminosalicylic acid is orally active .
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- HY-10446S1
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Pralatrexate- 13C5, 15N is the 13C- and 15N-labeled Pralatrexate (HY-10446). 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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| Cat. No. |
Product Name |
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Classification |
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- HY-10446
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Alkynes
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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-10446S1
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Alkynes
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Pralatrexate- 13C5, 15N is the 13C- and 15N-labeled Pralatrexate (HY-10446). 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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