DHFR

Cat. No.

A43971

CAS No.

134-05-4

10-Formylfolic acid

10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase, an enzyme critical in the folate metabolic pathway. This compound has been shown to exhibit significant biological activity, making it a valuable tool in cancer research. Its role as a potential early indicator of leukemia highlights its importance in diagnostic applications and therapeutic investigations targeting folate-dependent processes.

Cat. No.

A43972

CAS No.

2757070-32-7

Fluorofolin

Fluorofolin is a potent dihydrofolate reductase (DHFR) inhibitor, demonstrating an IC50 of 2.5 nM. This compound exhibits significant antimicrobial activity against Pseudomonas aeruginosa, making it a valuable reagent for research in antibacterial drug development and mechanisms of resistance. Fluorofolin is suitable for studies involving folate metabolism and has potential applications in exploring therapeutic strategies targeting DHFR-related pathways.

Cat. No.

A43973

CAS No.

6866-87-1

Phomarin

Phomarin is a specific inhibitor of dihydrofolate reductase (DHFR), an enzyme critical for folate metabolism. It demonstrates potential antimalarial activity, making it a valuable tool for research in malaria treatment and prevention. Its mechanism of action supports further investigations into antifolate strategies and their implications for drug development.

Cat. No.

A43974

CAS No.

1142407-81-5

DHFR-IN-5

DHFR-IN-5 is a highly potent and orally bioavailable inhibitor of dihydrofolate reductase (DHFR), exhibiting a Ki value of 0.54 nM against the quadruple mutant strain of Plasmodium falciparum DHFR. This compound demonstrates significant anti-malarial activity, making it a valuable tool for research into malaria therapeutics and the study of resistance mechanisms in Plasmodium species.

Cat. No.

A43975

CAS No.

28459-40-7

10-Formyl-7,8-dihydrofolic acid

10-Formyl-7,8-dihydrofolic acid is a potent substrate for dihydrofolate reductase (DHFR) and aminoimidazolecarboxamide ribonucleotide transformylase. It plays a significant role in promoting the growth of leukemia cells and can effectively reverse growth inhibition caused by antifolate medications in folate-deficient environments. This compound is valuable for research applications focused on leukemia and related therapeutic strategies.

Cat. No.

A43977

CAS No.

73090-70-7

Epiroprim

Synonyms: Ro11-8958

Epiroprim is a selective inhibitor of dihydrofolate reductase (DHFR), a key enzyme in folate metabolism. It exhibits potent antibacterial activity against various Gram-positive bacterial strains, including staphylococci, enterococci, pneumococci, and streptococci. Epiroprim is commonly utilized in research applications focused on antimicrobial resistance and drug development strategies targeting bacterial infections.

Cat. No.

A43978

CAS No.

79483-69-5

Piritrexim isethionate

Synonyms: BW 301U isethionate; NSC 351521 isethionate

Piritrexim isethionate is a fat-soluble inhibitor of dihydrofolate reductase (DHFR), primarily used in the treatment of severe psoriasis. This compound exhibits comparable efficacy to methotrexate for psoriasis management, while potentially offering a reduced risk of hepatotoxicity. Its selective target and biological activity make it a valuable reagent for research focusing on autoimmune skin disorders and folate metabolism.

Cat. No.

A43979

CAS No.

43170-88-3

Methotrexate diethyl ester

Methotrexate diethyl ester is a potent inhibitor of dihydrofolate reductase (DHFR). This compound demonstrates significant biological activity in the context of T. cruzi infection and leukemia research, making it valuable for investigating therapeutic strategies in these disease areas. Its ability to inhibit DHFR underscores its potential applications in studies focusing on cancer and parasitic infections.

Cat. No.

A43980

CAS No.

27192-37-6

Zymosterone

Zymosterone is a biochemical reagent that targets dihydrofolate reductase (DHFR). It is converted into zymosterol, an essential intermediate in cholesterol biosynthesis, through the action of hydroxysteroid (17β) dehydrogenase 7 (HSD17B7). This transformation, further catalyzed by 3-keto sterol reductase (ERG27), is critical for the biosynthesis of ergosterol in yeast, facilitating studies in lipid metabolism and cellular function.

Cat. No.

A43981

CAS No.

64801-58-7

Methotrexate-γ-aspartate

Methotrexate-γ-aspartate is a potent dihydrofolate reductase inhibitor, exhibiting enhanced resistance to enzymatic cleavage compared to methotrexate-γ-glutamate. This compound is utilized in antibody-targeted liposome formulations, making it a valuable tool for research in leukemia treatment. Its unique properties support its role in studying folate metabolism and chemoresistance in cancer therapies.

Cat. No.

A43983

CAS No.

3077918-44-3

BION106

BION106 is a dihydrofolate reductase-thymidylate synthase (DHFR-TS) PROTAC degrader that effectively targets and degrades DHFR-TS. It demonstrates potent antimalarial activity against Plasmodium falciparum, with a Ki value of 2.68 nM and selective toxicity of 0.2 μM in parasite cells, while showing significantly reduced toxicity (>100 μM and 44.2 μM) in mammalian cells. BION106 is valuable for research on antimalarial therapies and the mechanisms underlying parasite survival.

Cat. No.

A43984

CAS No.

3032441-13-4

DHFR-IN-9

DHFR-IN-9 is a potent inhibitor of dihydrofolate reductase (DHFR), critically involved in purine and thymidylate biosynthesis, playing a significant role in cellular proliferation and growth. This compound demonstrates robust antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 with an IC50 of 0.25 μg/mL, as well as notable anti-infective effects in mouse models of systemic and thigh infections. Additionally, DHFR-IN-9 exhibits superior anticancer efficacy compared to paclitaxel in a mouse breast cancer model, administered at 2.5 mg/kg every three days.

Cat. No.

A43985

CAS No.

3032441-09-8

DHFR-IN-8

DHFR-IN-8 is a potent dihydrofolate reductase (DHFR) inhibitor that disrupts purine and thymidylate biosynthesis, thereby impeding cell proliferation and growth. This compound exhibits significant antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300, with an IC50 value of 15.6 ng/mL. DHFR-IN-8 is applicable in research focused on tackling systemic infections and thigh infections in murine models.

Cat. No.

A43990

CAS No.

2941327-87-1

DHFR-IN-22

DHFR-IN-22 is a potent inhibitor of Dihydrofolate Reductase (DHFR), classified as a 2,4-diaminopyrimidine compound. It demonstrates remarkable inhibitory activity against purified DHFR and key non-tuberculous mycobacterial species, including Mycobacterium avium and Mycobacterium abscessus, with IC50 values of 1.1 nM and 6.3 nM, respectively, and MIC values of 1.5 μg/mL and 0.1 μg/mL, respectively. In contrast, it exhibits a significantly higher IC50 of 2100 nM against human DHFR. DHFR-IN-22 is valuable for investigating therapeutic strategies to address NTM infections.

Cat. No.

A43991

CAS No.

52454-37-2

10-Deazaaminopterin

10-Deazaaminopterin is a potent inhibitor of dihydrofolate reductase (DHFR), an essential enzyme involved in folate metabolism. This compound has demonstrated significant anti-tumor activity and is primarily utilized in cancer research to investigate its effects on cellular proliferation and metabolism. Its application is particularly relevant in studies focusing on advanced cancer therapies and folate-dependent biochemical pathways.

Cat. No.

A43992

CAS No.

3077918-47-6

PROTAC DHFR Degrader-1

PROTAC DHFR Degrader-1 is a selective PROTAC degrader that targets the dihydrofolate reductase-thymidylate synthase (DHFR-TS) complex of Plasmodium falciparum, exhibiting a Ki of 2.01 nM. This compound specifically degrades the parasite's DHFR without affecting human DHFR, effectively inhibiting the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 is suitable for research focused on malaria and the molecular mechanisms related to Plasmodium falciparum.

Cat. No.

A43995

CAS No.

1088704-78-2

DHFR-IN-24

DHFR-IN-24 is a dihydrofolate reductase (DHFR) inhibitor with a benzothiazole structure. This compound exhibits intrinsic antibacterial activity against Gram-positive and Gram-negative bacteria. Additionally, it demonstrates a synergistic effect when combined with photodynamic therapy (PDT), enhancing antibacterial efficacy against multidrug-resistant pathogens. Research applications include studying bacterial resistance mechanisms and developing novel antibacterial therapies.

Cat. No.

A43996

CAS No.

1142407-60-0

DHFR-IN-5 hydrochloride

DHFR-IN-5 hydrochloride is a potent inhibitor of dihydrofolate reductase (DHFR), exhibiting a Ki value of 0.54 nM against quadruple mutant Plasmodium falciparum DHFR. This compound demonstrates significant anti-malarial activity, making it a valuable tool for research in malaria treatment and drug development targeting DHFR pathways.

Cat. No.

A43997

CAS No.

41927-06-4

DHFR-IN-19

DHFR-IN-19 is a selective inhibitor of dihydrofolate reductase (DHFR) specifically targeting Trypanosoma brucei. With a Ki value of 9 nM, DHFR-IN-19 demonstrates significant antiparasitic activity, exhibiting an EC50 of 14.5 μM. This compound serves as a valuable tool for research into treatments for diseases caused by Trypanosoma brucei, particularly in the context of potential therapeutic applications against African sleeping sickness.

Cat. No.

A43998

CAS No.

118675-83-5

DDPO

DDPO is a potent inhibitor of dihydrofolate reductase (DHFR) with an IC50 of 0.035 µM. This compound demonstrates significant anticancer activity by inhibiting the growth of L1210 and WI-L2 cell lines, with IC50 values of 5 µM and 0.28 µM, respectively. DDPO is primarily used in research applications focusing on cancer therapeutics and DHFR-related pathways.

Cat. No.

A44017

CAS No.

5854-11-5

CB 3705

CB 3705 is a potent inhibitor of dihydrofolate reductase (DHFR) and thymidylate synthetase (TS). This compound demonstrates significant anti-cancer activity, exhibiting ID50 values of 4.77 μM against L1210 cells and 408 μM against the mutant L1210:C15 cell line. Its inhibition of key enzymes involved in nucleotide synthesis makes CB 3705 a valuable tool for cancer research and drug development.

Cat. No.

A48341

CAS No.

56518-41-3

Brodimoprim

Synonyms: Ro 10-5970

Brodimoprim is a potent dihydrofolate reductase inhibitor with broad-spectrum antibacterial activity. As an orally active trimethoprim analogue, it exhibits significant efficacy against various gram-negative and gram-positive bacteria. This compound is valuable for research applications in studying bacterial resistance and the mechanisms of folate metabolism.

Cat. No.

A48348

CAS No.

56066-63-8

Aditoprime

Synonyms: Aditoprim

Aditoprime is a selective inhibitor of bacterial dihydrofolate reductase (DHFR), demonstrating IC50 values of 47 nM and 520 nM for E. coli and L. casei DHFR, respectively. By inhibiting the conversion of dihydrofolic acid to tetrahydrofolic acid, Aditoprime effectively impairs bacterial folate synthesis. This compound exhibits broad-spectrum antibacterial activity and possesses favorable pharmacokinetic properties, making it a useful reagent in microbiological research and antibiotic development studies.

Cat. No.

A48456

CAS No.

82952-64-5

Trimetrexate glucuronate

Synonyms: CI-898 glucuronate

Trimetrexate glucuronate is a potent inhibitor of dihydrofolate reductase, effectively functioning as a folic acid antagonist. By disrupting the synthesis of purine nucleotides and thymidylate, it significantly impairs DNA and RNA synthesis. This compound exhibits potential antitumor activity and is also applicable in the treatment and inhibition of Pneumocystis carinii pneumonia, making it a valuable tool in cancer research and infectious disease studies.

Cat. No.

A48751

CAS No.

29606-06-2

Ro 20-0657/000

Ro 20-0657/000 is a dihydrofolate reductase inhibitor that serves as a metabolite of trimethoprim. This compound exhibits antibacterial activity, making it relevant for both human and veterinary medical applications. Ro 20-0657/000 is utilized in research to investigate the mechanisms of folate metabolism and the potential therapeutic effects of dihydrofolate reductase inhibition.