Date published: 2025-12-5

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DHFR Inhibitors

DHFR inhibitors, known as Dihydrofolate Reductase inhibitors, constitute a vital category of chemical compounds with substantial implications in the fields of medicinal chemistry and biochemistry. These inhibitors are meticulously designed to interact with and modulate the activity of the enzyme dihydrofolate reductase (DHFR). DHFR plays a central role in the complex folate metabolic pathway. Its primary function involves catalyzing the conversion of dihydrofolate (DHF) into tetrahydrofolate (THF), a crucial co-factor necessary for numerous biochemical processes. These processes include nucleotide synthesis, which forms the structural basis of DNA and RNA, as well as amino acid production. Consequently, the inhibition of DHFR disrupts this intricate metabolic cascade, ultimately influencing DNA replication and cellular proliferation. Within the realm of DHFR inhibitors, a diverse spectrum of structurally distinct compounds exists, including well-known examples like methotrexate, trimethoprim, and pyrimethamine. These inhibitors collectively share a common mechanism of action, characterized by their ability to bind to the active site of the DHFR enzyme. This binding effectively impedes the enzyme's catalytic function, disrupting the conversion of DHF into THF. This leads to a shortage of THF within the cellular environment, thereby affecting the synthesis of essential biomolecules, particularly nucleotides. Consequently, cell growth and division are compromised. Due to their capacity to selectively target rapidly dividing cells, DHFR inhibitors have garnered significant attention across various applications, including their use against microbial infections. Their intricate role in disrupting crucial cellular processes underscores their paramount importance in scientific research.

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Items 11 to 19 of 19 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Murexide

3051-09-0sc-215401
5 g
$26.00
(0)

Murexide acts as a potent inhibitor of dihydrofolate reductase (DHFR) through its unique ability to form stable complexes with the enzyme. Its structural features allow for specific electrostatic interactions and coordination with metal ions, enhancing binding affinity. The compound's distinct resonance stabilization contributes to its reactivity, influencing the enzyme's catalytic pathway. This dynamic interaction alters the enzyme's conformational landscape, impacting overall enzymatic activity and efficiency.

Raltitrexed

112887-68-0sc-219933
10 mg
$143.00
(0)

Raltitrexed functions as a selective inhibitor of dihydrofolate reductase (DHFR) by mimicking the natural substrate, thereby disrupting the enzyme's active site. Its unique structural conformation facilitates strong hydrogen bonding and hydrophobic interactions, which stabilize the enzyme-inhibitor complex. This compound exhibits a slow dissociation rate, leading to prolonged inhibition and altered enzyme kinetics, ultimately affecting the metabolic flux within folate-dependent pathways.

Sulfaguanidine

57-67-0sc-251083
sc-251083A
25 g
100 g
$51.00
$92.00
(0)

Sulfaguanidine acts as a competitive inhibitor of dihydrofolate reductase (DHFR), characterized by its ability to form specific interactions with the enzyme's active site. Its unique sulfonamide group enhances binding affinity through electrostatic interactions, while its structural rigidity promotes effective steric hindrance. This compound exhibits distinct reaction kinetics, leading to a notable decrease in enzyme activity and subsequent modulation of folate metabolism, impacting cellular processes reliant on this pathway.

Trimethoprim-13C3

1189970-95-3sc-220336
500 µg
$800.00
(0)

Trimethoprim-13C3 exhibits a distinctive mechanism of action as a dihydrofolate reductase (DHFR) inhibitor, characterized by its isotopic labeling that enhances tracking in metabolic studies. The compound's structural conformation allows for specific hydrogen bonding and hydrophobic interactions within the enzyme's active site, leading to a pronounced decrease in enzymatic activity. This selective inhibition alters the dynamics of folate metabolism, providing insights into enzyme kinetics and regulatory pathways.

Trimethoprim lactate salt

23256-42-0sc-237332
250 mg
$180.00
2
(1)

Trimethoprim lactate salt functions as a potent inhibitor of dihydrofolate reductase (DHFR) through its selective binding to the enzyme's active site. The compound's unique lactate moiety contributes to its solubility and stability, facilitating enhanced interaction with DHFR. Its molecular structure allows for optimal alignment within the enzyme, promoting effective competition with the natural substrate. This results in altered reaction kinetics, significantly impacting the folate synthesis pathway and associated metabolic processes.

Sulfameter

651-06-9sc-212975
100 mg
$330.00
(0)

Sulfameter functions as a dihydrofolate reductase (DHFR) inhibitor, showcasing unique interactions with the enzyme's active site. Its molecular structure facilitates specific electrostatic interactions and steric hindrance, effectively disrupting substrate binding. The compound's kinetic profile reveals a competitive inhibition mechanism, influencing the rate of folate reduction. This modulation of enzymatic activity offers a deeper understanding of metabolic regulation and enzyme-substrate dynamics.

7-Hydroxy Methotrexate Sodium Salt

5939-37-7sc-217447A
sc-217447
500 µg
1 mg
$194.00
$357.00
11
(1)

7-Hydroxy Methotrexate Sodium Salt acts as a dihydrofolate reductase (DHFR) inhibitor, characterized by its ability to form hydrogen bonds with key amino acid residues in the enzyme's active site. This compound exhibits a unique conformational flexibility that enhances its binding affinity, leading to altered reaction kinetics. Its distinct solubility properties allow for effective interaction in various biochemical environments, providing insights into enzyme inhibition mechanisms and metabolic pathways.

Succinylsulfathiazole

116-43-8sc-224293
sc-224293A
100 g
500 g
$215.00
$1020.00
(0)

Succinylsulfathiazole functions as a dihydrofolate reductase (DHFR) inhibitor, distinguished by its ability to engage in hydrophobic interactions with the enzyme's active site. This compound features a unique structural arrangement that facilitates specific electrostatic interactions, influencing the enzyme's catalytic efficiency. Its kinetic profile reveals a competitive inhibition mechanism, providing a nuanced understanding of substrate dynamics and enzyme regulation in metabolic processes.

Difluoromethylornithine

70052-12-9sc-204723
sc-204723A
sc-204723B
sc-204723C
sc-204723D
sc-204723E
10 mg
25 mg
100 mg
250 mg
1 g
5 g
$58.00
$130.00
$158.00
$311.00
$964.00
$4726.00
2
(1)

Eflornithine is an anti-parasitic drug that inhibits DHFR in Trypanosoma brucei, causing cell death in the parasite.