MTHFSD Inhibitors
MTHFSD inhibitors represent a class of chemical compounds that target the enzyme methenyltetrahydrofolate synthetase dehydrogenase (MTHFSD). This enzyme plays a crucial role in the folate cycle, a vital biochemical pathway responsible for various cellular processes such as the biosynthesis of nucleotides and the regulation of methylation reactions. MTHFSD, specifically, is involved in catalyzing the conversion of methenyl-tetrahydrofolate (MTHF) into its various forms, including methylene-tetrahydrofolate, which is essential for the synthesis of purines and thymidylate, important precursors for DNA replication and repair. Inhibitors of MTHFSD disrupt this enzyme's activity, leading to a downstream reduction in the availability of one-carbon units needed for biosynthetic pathways and other cellular processes, thus impacting nucleotide biosynthesis and methylation balance.
Chemically, MTHFSD inhibitors are designed to interfere with the enzyme's active site or its cofactor interactions, preventing its catalytic activity. They may act by mimicking the natural substrate of the enzyme, competitively binding to the active site, or by inducing allosteric effects that change the enzyme's conformation, rendering it inactive. These inhibitors often contain structural motifs that closely resemble the intermediate states of folate derivatives in the catalytic cycle, allowing them to bind with high specificity and affinity to the enzyme. Through this precise inhibition mechanism, MTHFSD inhibitors can serve as powerful tools in studying the folate cycle's biochemistry and its broader implications on cellular function, including epigenetic regulation, cell proliferation, and energy metabolism.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Methotrexate | 59-05-2 | sc-3507 sc-3507A | 100 mg 500 mg | $94.00 $213.00 | 33 | |
Methotrexate is a competitive inhibitor of dihydrofolate reductase (DHFR), leading to decreased availability of tetrahydrofolate, the substrate for other folate-dependent enzymes, which could potentially downregulate MTHFSD expression due to folate depletion. | ||||||
Pyrimethamine | 58-14-0 | sc-208190 sc-208190A sc-208190B | 1 g 5 g 25 g | $80.00 $238.00 $825.00 | 5 | |
Pyrimethamine binds selectively to parasitic DHFR. While it's less selective for human DHFR, high doses can decrease human folate metabolism, potentially reducing MTHFSD expression through folate scarcity. | ||||||
Trimethoprim | 738-70-5 | sc-203302 sc-203302A sc-203302B sc-203302C sc-203302D | 5 g 25 g 250 g 1 kg 5 kg | $67.00 $161.00 $255.00 $721.00 $3401.00 | 4 | |
Trimethoprim selectively inhibits bacterial DHFR over the human form. However, at high concentrations, it can inhibit human DHFR, which may lead to a decrease in MTHFSD expression due to reduced folate concentration. | ||||||
Raltitrexed | 112887-68-0 | sc-219933 | 10 mg | $146.00 | ||
Raltitrexed is a specific thymidylate synthase inhibitor, which may lead to a reduction in thymidine monophosphate levels, a condition that could secondarily downregulate MTHFSD expression as part of a cellular response to nucleotide imbalance. | ||||||
Sulfamethoxazole | 723-46-6 | sc-208405 sc-208405A sc-208405B sc-208405C | 10 g 25 g 50 g 100 g | $37.00 $55.00 $69.00 $109.00 | 5 | |
Sulfamethoxazole competes with para-aminobenzoic acid, interfering with bacterial folate synthesis. This interference could theoretically translate to a reduced human folate pool, potentially decreasing MTHFSD expression. | ||||||
Aminopterin | 54-62-6 | sc-202461 | 50 mg | $102.00 | 1 | |
Aminopterin is a derivative of folic acid that inhibits DHFR, leading to depleted folate reserves. This depletion could result in the downregulation of MTHFSD expression due to insufficient substrate availability for folate-dependent processes. | ||||||
8-(4-Amino-1-methylbutylamino)-6-methoxyquinoline | 90-34-6 | sc-483239 | 1 g | $360.00 | 1 | |
8-(4-Amino-1-methylbutylamino)-6-methoxyquinoline disrupts the electron transport in parasites. In human cells, its oxidative stress might contribute to the reduction of nucleotide pools, which could hypothetically lead to decreased MTHFSD expression. | ||||||
Hydroxyurea | 127-07-1 | sc-29061 sc-29061A | 5 g 25 g | $78.00 $260.00 | 18 | |
Hydroxyurea targets ribonucleotide reductase, restricting DNA synthesis. This restriction could lead to a cellular environment that downregulates MTHFSD expression as part of a broader response to DNA replication stress. | ||||||
Fluorouracil | 51-21-8 | sc-29060 sc-29060A | 1 g 5 g | $37.00 $152.00 | 11 | |
Fluorouracil is an analog of uracil and inhibits thymidylate synthase, leading to a decrease in thymidine synthesis. Reduced thymidine availability could lead to the downregulation of MTHFSD expression. | ||||||
3′-Azido-3′-deoxythymidine | 30516-87-1 | sc-203319 | 10 mg | $61.00 | 2 | |
3′-Azido-3′-deoxythymidine is a nucleoside analog reverse transcriptase inhibitor that can incorporate into the growing DNA strand, leading to chain termination. This inhibition could theoretically reduce MTHFSD expression by disrupting RNA processing. | ||||||