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antifolate activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antifolate (12) Amino Acid Derivatives (1) Apoptosis (4) Bacterial (3) Bcl-2 Family (3) Caspase (3) Dihydrofolate reductase (DHFR) (3) Parasite (3)
By Research Areas:	Cancer (12) Infection (6) Inflammation/Immunology (1)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Peptides

Click Chemistry

Targets Recommended: Antifolate

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107981

LSN 3213128 1 Publications Verification	Antifolate	Cancer
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC₅₀ of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity .

HY-126878

11-Oxahomoaminopterin	Antifolate	Infection Cancer
11-Oxahomoaminopterin shows antifolate activity and inhibits Lactobacillus casei DHFFZ with antimicrobial and antitumor activities .

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-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-W047788

H-Dab(Boc)-OH	Amino Acid Derivatives	Others
H-Dab(Boc)-OH is an amino acid derivative with a Boc protecting group, which can be used to synthesize methotrexate (MTX) analogs with antitumor and antifolate activities .

HY-105934A

Ketotrexate sodium Emofolin sodium; 5-methyltetrahydrohomofolate sodium; NSC 139490 sodium	Antifolate	Inflammation/Immunology Cancer
Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases .

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-13714

Nolatrexed AG 337 free base	Others	Others
Nolatrexed (AG 337 free base) is a compound with antifolate activity, high oral bioavailability, and major toxicity at inhibitory doses is gastrointestinal reactions. It can be safely taken orally at specific doses for inhibition, with effects on platelets and neutrophils.

HY-154807

DQn-1	Bacterial	Infection
DQn-1 is a potent antifolate with activity against Mycobacterium tuberculosis (Mtb) (MIC₉₀=0.03 µM). DQn-1 directly inhibits DHFR enzyme activity, with IC₅₀s of 8.7 and 7.6 nM for Mtb and human DHFR enzyme, respectively .

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-10824A

Talotrexin monoammonium PT523 monoammonium	Dihydrofolate reductase (DHFR) Antifolate	Cancer
Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic *antifolate. Talotrexin monoammonium is a reduced folate* carrier (RFC)** specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth .

HY-13617

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

HY-151935

Antileishmanial agent-13	Parasite	Infection
Antileishmanial agent-13 is a quinoline-isatin hybrid, acts as an antileishmanial agent against L. Major Leishmania strain. Antileishmanial agent-13 acquires the antileishmanial activity via the anti-folate mechanism. Antileishmanial agent-13 has potent inhibition against both promastigote and amastigote forms with IC₅₀s of 0.604 μM and 0.508 μM, respectively .

HY-14521

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

HY-14521B

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

HY-10446

Pralatrexate Maximum Cited Publications 7 Publications Verification	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-14521A

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

HY-155845

Antileishmanial agent-21	Parasite	Infection
Antileishmanial agent-21 (compound 4e) is an antileishmanial agent that targets the Leishmania pteridine reductase 1 (Lm-PTR1). Antileishmanial agent-21 has an anti-folate mechanism, and folic acid and leucovorin can reverse the anti-leishmanial activity of Antileishmanial agent-21. Antileishmanial agent-21 inhibits the Chloroquine (HY-17589A)-resistant strain of Plasmodium falciparum (RKL9) with an IC₅₀ of 0.0198-0.096 μM .

HY-155846

Antileishmanial agent-22	Parasite Bacterial	Infection
Antileishmanial agent-22 (compound 15b) is a parasite inhibitor and an antibacterial agent, with antileishmanial, antimalarial, and anti-tubercular activities. Antileishmanial agent-22 inhibits leishmanial (IC₅₀=0.408 μM) based on antifolate mechanism. And, Antileishmanial agent-22 inhibits Folic acid and Folinic acid at 100 μM with inhibitory rates of 88% and 94%, respectively. Antileishmanial agent-22 inhibits P. berghei in vivo and in vitro, with 96.67% suppression under 48.4 μM/kg/day and 0.038 μM (IC₅₀), respectively. Moreover, Antileishmanial agent-22 inhibits M. tuberculosis with MIC of 28.44 μM .

Cat. No.	Product Name	Target	Research Area

HY-W047788

H-Dab(Boc)-OH	Amino Acid Derivatives	Others
H-Dab(Boc)-OH is an amino acid derivative with a Boc protecting group, which can be used to synthesize methotrexate (MTX) analogs with antitumor and antifolate activities .

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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