dhfr

DHFR-IN-3 (7-bromoquinazoline-2,4-diamine) is a dihydrofolate reductase (DHFR) inhibitor.

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumor activity, which also inhibits EGFR and HER2, and is useful for studying pancreatic cancer.

Piritrexim (BW 301U) is an orally available fat-soluble dihydrofolate reductase inhibitor with pulmonary toxicity used in the study of uroepithelial carcinoma and metastatic breast cancer.

Methotrexate Diglutamate Small molecule compound present in the liver that acts as a partially purified human dihydrofolate reductase inhibitor.

Talotrexin ammonium is a non-polyglutamic acid antifolate. Talotrexin ammonium inhibits tumor growth by targeting dihydrofolate reductase (DHFR), thereby improving anti-tumor activity in a wide range of cancer models, helping to inhibit tumor growth.

P 218 is a novel DHFR inhibitor with antimalarial activity and antifolate effects and can be used to study Buruli ulcer.

Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).

Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

Urea (Carbonyldiamide) is formed in the liver from ammonia produced by the deamination of amino acids. It is the principal end metabolite of protein catabolism and accounts for about one-half of the total urinary solids.

Sulfadoxine (Sulphadoxine) is a broad-spectrum sulfanilamide and a synthetic analog of para-aminobenzoic acid (PABA) with bacteriostatic and antimalarial properties.

Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.

Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.

Gentamicin sulfate (SCH9724) is a broad-spectrum, orally administered aminoglycoside antibiotic that exhibits inhibitory activity against aerobic Gram-negative bacteria by interfering with mRNA translation.

WR99210 (BRL 6231 free base) is an orally available dihydrofolate reductase (DHFR) inhibitor with antiparasitic activity, often used in combination with dapsone to study Mycobacterium avium complex (MAC).

10-Formylfolic acid is a novel and potent inhibitor of dihydrofolate reductase, which can be used in leukemia research.

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.

4′-DTMP (4-Demethyltrimethoprim) is a potent DHFR inhibitor with antimicrobial activity that induces additional local interactions with the enzyme and inhibits Escherichia coli.

VEGFR-2/DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2/DHFR-IN-2 holds promise for cancer research [1].

VEGFR-2/DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

DHFR-IN-5, an orally active and potent inhibitor of dihydrofolate reductase (DHFR), exhibits a K_i value of 0.54 nM against the quadruple mutant Plasmodium falciparum DHFR, demonstrating anti-malarial activity.

DHFR-IN-8 (compound 6r), a dihydrofolate reductase (DHFR) inhibitor, disrupts purine and thymidylate biosynthesis critical for cell proliferation and growth. This compound effectively suppresses methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 with an IC50 of 15.6 ng/mL in mouse models of systemic and thigh infections [1].

DHFR-IN-9 (compound 8A), a dihydrofolate reductase (DHFR) inhibitor, impedes purine and thymidylate biosynthesis, pivotal in cell proliferation and growth. It demonstrates potency against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 with an IC50 of 0.25 μg/mL and exhibits anti-infective properties in mouse systemic and thigh infection models at doses of 2.5 mg/kg and 5 mg/kg administered intraperitoneally (ip). Furthermore, DHFR-IN-9 shows greater anticancer efficacy in a mouse breast cancer model compared to paclitaxel (Y-B0015), at a regimented dosage of 2.5 mg/kg ip every three days [1].