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DHFR+Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (4) Antifolate (37) Apoptosis (4) Bacterial (17) Cytochrome P450 (1) Dihydrofolate reductase (DHFR) (30) DNA/RNA Synthesis (11) Drug Metabolite (1) EGFR (4) Isotope-Labeled Compounds (7) Nucleoside Antimetabolite/Analog (1) Parasite (26) Reference Standards (10) STAT (7)
By Research Areas:	Cancer (30) Cardiovascular Disease (1) Endocrinology (1) Infection (50) Inflammation/Immunology (4)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18062

Pyrimethamine Maximum Cited Publications 13 Publications Verification 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-10446

Pralatrexate 5+ Cited Publications	Antifolate Apoptosis	Cancer
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.

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-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-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-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-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-107033

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

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-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-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-106434

Piritrexim 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

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-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-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-18062R

Pyrimethamine (Standard) 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

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-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-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-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-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-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-169211

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

HY-149699

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

HY-161063

DHFR-IN-14	Dihydrofolate reductase (DHFR)	Cancer
DHFR-IN-14 (compound 32) is a pyrimethamine (Pyr)-type, dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity .

HY-107033R

Tetroxoprim (Standard) HE 781 (Standard)	Reference Standards Antifolate	Infection Inflammation/Immunology
Tetroxoprim (Standard) is the analytical standard of Tetroxoprim. This product is intended for research and analytical applications. Tetroxoprim is an antimicrobial *DHFR* inhibitor .

HY-117791

(R)-Pralatrexate	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-121207

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

HY-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-118251

PD130883	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-B0806AS

Proguanil-d4 hydrochloride	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-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-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-B1902R

Diaveridine (Standard) 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-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-111202R

Pyributicarb (Standard) TSH-888 (Standard)	Reference Standards Cytochrome P450	Inflammation/Immunology
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 .

HY-B0806R

Proguanil (Standard)	Reference Standards Parasite Antifolate	Infection
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 .

HY-B0806AR

Proguanil hydrochloride (Standard)	Reference Standards Parasite Antifolate	Infection
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 .

HY-B0806AS1

Proguanil-d6 hydrochloride	Isotope-Labeled Compounds Parasite Antifolate	Infection
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-N10791

Neobritannilactone B	Others	Infection
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-B1902S

Diaveridine-d6 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 K_i of 11.5 nM for the wild type DHFR and also an antibacterial agent .

HY-143408

OYYF-175	Bacterial	Infection
OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC₅₀ of 2.36 nM for **Escherichia coli DHFR**. OYYF-175 exhibits potent broad-spectrum antibacterial activities, especially against multi-drug resistant Gram-Negative-strains .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

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 .

Cat. No.	Product Name	Chemical Structure

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-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-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-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 .

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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