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DHFR inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Dihydrofolate reductase (DHFR) (56) Akt (1) Antibiotic (11) Antifolate (55) Apoptosis (11) Autophagy (11) Bacterial (37) Cytochrome P450 (2) Deubiquitinase (1) DNA/RNA Synthesis (11) Drug Metabolite (1) EGFR (9) Endogenous Metabolite (1) Ferroptosis (1) Fungal (6) Glutathione Peroxidase (1) Isotope-Labeled Compounds (11) Nucleoside Antimetabolite/Analog (1) Parasite (29) Reactive Oxygen Species (ROS) (1) Reference Standards (16) STAT (7) Thymidylate Synthase (1) VEGFR (2)
By Research Areas:	Cancer (56) Cardiovascular Disease (1) Endocrinology (1) Infection (76) Inflammation/Immunology (14) Neurological Disease (1)
Click Chemistry:	Alkynes (1)

121

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Dihydrofolate reductase (DHFR)

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 K_i 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

Pyrimethamine 10+ Cited Publications 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

Pemetrexed disodium Maximum Cited Publications 39 Publications Verification LY231514 disodium	Antifolate Autophagy Apoptosis	Cancer
Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is 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-10373

Trimetrexate 2 Publications Verification 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

4-Aminosalicylic acid 1 Publications Verification	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

Pemetrexed disodium hemipenta hydrate Maximum Cited Publications 39 Publications Verification LY231514 disodium hemipenta hydrate	Antifolate Autophagy Apoptosis	Infection Neurological Disease Inflammation/Immunology Cancer
Pemetrexed (LY231514) disodium hemipenta hydrate is a CNS-penetrant antifolate, the K_i 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

Pemetrexed disodium heptahydrate Maximum Cited Publications 39 Publications Verification LY231514 disodium heptahydrate	Antifolate Autophagy	Cancer
Pemetrexed disodium heptahydrate is a novel antifolate, the K_i 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-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 .

HY-B0806

Proguanil 3 Publications Verification	Parasite Antifolate	Infection
Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .

HY-153007

DHFR-IN-5	Dihydrofolate reductase (DHFR)	Infection
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a K_i value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity .

HY-12784A

Cycloguanil hydrochloride 3 Publications Verification 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-B0806A

Proguanil hydrochloride 3 Publications Verification	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-162475

Fluorofolin	Dihydrofolate reductase (DHFR) Bacterial	Infection
Fluorofolin is a dihydrofolate reductase (DHFR) inhibitor with an IC₅₀ of 2.5 nM. Fluorofolin exhibits significant activity against P. aeruginosa .

HY-B1902

Diaveridine EGIS-5645	Antifolate Bacterial	Infection
Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a K_i of 11.5 nM for the wild type DHFR and also an antibacterial agent.

HY-107033

Tetroxoprim HE 781	Antifolate	Infection Inflammation/Immunology
Tetroxoprim is an antimicrobial *DHFR* inhibitor .

HY-169790

Phomarin	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

DHFR-IN-3	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-W587663

4′-DTMP	Dihydrofolate reductase (DHFR)	Infection
4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFR ^WT) and 34.3 nM (DHFR ^L28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli .

HY-116387A

WR99210 hydrochloride 4 Publications Verification 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

DHFR-IN-4	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-156859A

NSC309401	Bacterial	Infection
NSC309401 is an inhibitor of E. coli *DHFR* (IC₅₀: 189 nM, K_D: 14.57 nM) .

HY-139743

Aditoprime 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-179415

DHFR-IN-24	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-12784

Cycloguanil 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-12784AR

Cycloguanil hydrochloride (Standard) 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-10373A

Trimetrexate trihydrochloride 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-10373B

Trimetrexate isethionate 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-149200

Lysine-methotrexate	Antifolate	Inflammation/Immunology
Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor .

HY-119613

Clociguanil BRL 50216	Parasite Dihydrofolate reductase (DHFR)	Infection Cardiovascular Disease
Clociguanil (BRL 50216), a *DHFR* inhibitor (IC₅₀: 55.6 nM), is an antimalarial agent. Clociguanil has sympathomimetic and antiarrhythmic action .

HY-160254

1954U89	Dihydrofolate reductase (DHFR)	Cancer
1954U89 is a potent, lipid-soluble and orally active inhibitor of dihydrofolate reductase (DHFR). 1954U89 exhibits anticancer activity .

HY-116039

Epiroprim 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-10824B

Talotrexin ammonium PT523 ammonium	Dihydrofolate reductase (DHFR) Antifolate	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 .

HY-18062S

Pyrimethamine-d3	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-B0806S1

Proguanil-d4	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

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 .

HY-122289

Metioprim	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-149699

DHFR-IN-12	Dihydrofolate reductase (DHFR)	Infection
DHFR-IN-12 (Compound 5c) is a *DHFR* inhibitor which has good antibacterial activity .

HY-139743R

Aditoprime (Standard) 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-177337

N-Didesmethyladitoprim 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-161064

DHFR-IN-15	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-163725

DHFR-IN-18	Dihydrofolate reductase (DHFR)	Cancer
DHFR-IN-18 (compound 19D) is a *DHFR* inhibitor. DHFR-IN-18 can be used in anti-leukemia research .

HY-156412

DHFR-IN-10	Bacterial	Infection
DHFR-IN-10 (compound 4c) is a potent *DHFR* inhibitor, with an IC₅₀ of 4.21 μM for M. tuberculosis DHFR enzyme. DHFR-IN-10 exhibits potent antituberculosis efficiency .

HY-153007A

DHFR-IN-5 hydrochloride	Dihydrofolate reductase (DHFR)	Infection
DHFR-IN-5 hydrochloride is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a K_i value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 hydrochloride shows anti-malaria activity .

HY-169211

DHFR-IN-21	Dihydrofolate reductase (DHFR)	Cancer
DHFR-IN-21 (compund 5p) is a dihydrofolate reductase (DHFR) inhibitor .

HY-156414

DHFR-IN-11	Dihydrofolate reductase (DHFR)	Infection
DHFR-IN-11 (compound 6b) is inhibitor of *DHFR, and has inhibitory potency versus M. tuberculosis* *DHFR* enzyme with IC₅₀ values 5.70 μM .

HY-161010

DHFR-IN-13	Dihydrofolate reductase (DHFR)	Infection
DHFR-IN-13 (Compd Hit8) is an active R. solani DHFR inhibitor with an IC₅₀ value of 10.2 μM. DHFR-IN-13 has selectivity of inhibition against human DHFR with an IC₅₀ value of 227.7 μM. DHFR-IN-13 also is a fungicide. DHFR-IN-13 has high antifungal activity against R. solani with EC₅₀ value of 38.2 mg/L .

HY-137439

Fanotaprim 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-172897

EGFR/DHFR-IN-2	EGFR Dihydrofolate reductase (DHFR) Apoptosis Cytochrome P450	Cancer
EGFR/DHFR-IN-2 (9b) is a dual h-DHFR/EGFR ^TK inhibitor, with IC₅₀ values of 0.192 μM and 0.109 μM for h-DHFR and EGFR, respectively. EGFR/DHFR-IN-2 (9b) halts the cell cycle at the G1/S phase and induces apoptosis. EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. EGFR/DHFR-IN-2 (9b) can be used in the cancer research .

HY-168648

DNA Gyrase/DHFR-IN-1	Bacterial Fungal Dihydrofolate reductase (DHFR)	Infection
DNA Gyrase/DHFR-IN-1 is a dual inhibitor of bacterial DNA gyrase and *DHFR, with IC₅₀s of 182 μM and 3.90 μM for E. coli DNA gyrase and DHFR* respectively. DNA Gyrase/DHFR-IN-1 has bactericidal and antifungal activity .

HY-173220

DHFR-IN-23	Dihydrofolate reductase (DHFR) Apoptosis	Cancer
DHFR-IN-23 (compound 5) is a dual DNA binders/DHFR inhibitor, with an IC₅₀ of 0.08 μM for hDHFR. DHFR-IN-23 (compound 5) is also an apoptosis inducer. DHFR-IN-23 (compound 5) can be used for the research of ER+ breast cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-169790

Phomarin	Plantaginaceae Digitalis purpurea L. Quinones Structural Classification Anthraquinones Plants Source Classification	Dihydrofolate reductase (DHFR) Parasite Fungal
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-N10791

Neobritannilactone B	Zingiber officinale Roscoe Terpenoids Sesquiterpenes Plants Source Classification Zingiberaceae	Others
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 .

HY-N3764

Diosbulbin C	Terpenoids Diterpenoids Plants Dioscorea bulbifera Linn. Dioscoreaceae Source Classification	Akt Dihydrofolate reductase (DHFR) Endogenous Metabolite
Diosbulbin C is a diterpene lactone component, which can be extracted from traditional Chinese medicine Dioscorea bulbifera L.. Diosbulbin C possesses high anticancer activity in non-small cell lung cancer (NSCLC). Diosbulbin C could induce cell cycle arrest at G0/G1 phase in NSCLC. Diosbulbin C also inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of AKT, *DHFR, and TYMS* .

Cat. No.	Product Name	Chemical Structure

HY-18062S

Pyrimethamine-d3
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-B0806S1

Proguanil-d4
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-12784S

Cycloguanil-d6

1 Publications Verification

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

Cycloguanil-d4 hydrochloride

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

Cycloguanil-d6 hydrochloride

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-12784S1

Cycloguanil-d6 nitrate

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-B1902S

Diaveridine-d6
Diaveridine-d₆ (EGIS-5645-d₆) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a K_i of 11.5 nM for the wild type DHFR and also an antibacterial agent .

HY-B0806AS

Proguanil-d4 hydrochloride
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-B0806AS1

Proguanil-d6 hydrochloride
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 .

HY-10820S

Pemetrexed-d5
Pemetrexed-d₅ is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the K_i 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-10820AS

Pemetrexed-d5 disodium
Pemetrexed-d₅ disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is 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-W769288

Pemetrexed disodium-13C5
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 .

HY-I0447S

4-Aminosalicylic acid-d6
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 .

Cat. No.	Product Name		Classification

HY-10446

Pralatrexate 5+ Cited Publications		Alkynes
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a K_i 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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