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.

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

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

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.

Sulfameter (Sulfametoxydiazine) is a long-acting sulfonamide antibacterial agent used to treat urinary tract infections and leprosy.

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 wide-spectrum, aminoglycoside antibiotic used to inhibit protein synthesis in sensitive organisms.

Diaveridine (AI3-23935) (DVD) is a popular antibacterial synergist that is widely used in combination with sulfonamide. It has been reported to be genotoxic to mammalian cells, but more studies are required to clarify this.

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

Trioxsalen (Trioxysalen) is a furanocoumarin and a psoralen derivative, in conjunction with UV-A for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death.

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.

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

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.

DHFR-IN-20 (Compound LA1) is an inhibitor of dihydrofolate reductase (DHFR) targeting the malignant strains of the malaria parasite. It exhibits inhibition constants (Kis) of 0.16 nM, 0.30 nM, and 6.6 nM for PfDHFR-WT, PfDHFR-QM, and HsDHFR, respectively. Additionally, DHFR-IN-20 demonstrates antimalarial activity, with IC50 values of 1.4 nM against parasites carrying the wild-type (TM4 8.2) PfDHFR enzyme and 1.6 μM against those with the quadruple mutation (V1 S)PfDHFR.

DHFR-IN-21 (compound 5p) is an inhibitor of dihydrofolate reductase.

DNA Gyrase DHFR-IN-1 is a dual inhibitor targeting bacterial DNA gyrase and DHFR, with IC50 values of 182 μM and 3.90 μM against E. coli DNA gyrase and DHFR, respectively. This compound exhibits both bactericidal and antifungal activities.

DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase) inhibitor that falls under the category of 2,4-diaminopyrimidine compounds. It demonstrates significant inhibitory activity against isolated DHFR enzyme and major nontuberculous mycobacteria (NTM) species, specifically Mycobacterium avium and Mycobacterium abscessus. The compound has an IC50 of 1.1 nM and a MIC of 1.5 μg mL for M. abscessus, and an IC50 of 6.3 nM and a MIC of 0.1 μg mL for M. avium, while its IC50 for human DHFR is 2100 nM. DHFR-IN-22 may be promising for developing new strategies to combat NTM infections.

DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.

EGFR/DHFR-IN-2 (9b) is a dual inhibitor of h-DHFR/EGFR TK, exhibiting IC50 values of 0.192 μM for h-DHFR and 0.109 μM for EGFR. It causes cell cycle arrest at the G1/S phase and induces apoptosis. Additionally, EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. This compound can be utilized in cancer research.

DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor of MtDHFR, with an IC50 of 7 μM. The enzyme dihydrofolate reductase from M. tuberculosis (MtDHFR) holds high unexploited potential as a drug target due to its importance for pathogen survival. DHFR-IN-2 can be used for tuberculosis (TB) research [1].

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].

EGFR HER2 DHFR-IN-1 is a highly selective and potent anticancer compound targeting MCF-7 breast cancer cells, acting as a multi-inhibitor for EGFR HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. It induces cell cycle arrest at the G1 S phase and apoptosis in cells [1].