AICAR transformylase Inhibitors
AICAR Transformylase inhibitors encompass a diverse group of chemicals that primarily target the bifunctional enzyme ATIC, involved in purine biosynthesis. These inhibitors function through various mechanisms, including competitive inhibition, feedback inhibition, substrate mimicry, and indirect pathway interference. For instance, Methotrexate and Pemetrexed act as competitive inhibitors, resembling the enzyme's substrates and thus preventing normal enzyme function. Conversely, AICAR (Acadesine) itself, at high concentrations, serves as a feedback inhibitor, demonstrating the enzyme's ability to be regulated by its own substrate or related compounds.
These inhibitors are not uniform in their structure or origin. Some, like Leflunomide and Azathioprine, are synthetic compounds, while others, such as 6-Mercaptopurine and Thioguanine, are purine analogues. The diversity in their chemical structures corresponds to the variety in their modes of inhibition. For example Sulfamethoxazole and Trimethoprim indirectly inhibit the enzyme by interfering with the folate metabolism, crucial for purine synthesis. This indirect inhibition underscores the interconnected nature of metabolic pathways and how targeting one can influence another.
SEE ALSO...
| 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 an inhibitor of dihydrofolate reductase (DHFR) Inhibition of DHFR leads to the inhibition of AICAR transformylase | ||||||
Pemetrexed Disodium | 150399-23-8 | sc-219564 | 10 mg | $136.00 | 5 | |
Pemetrexed inhibits AICAR transformylase by mimicking the natural substrates of the enzyme, resulting in reduced purine synthesis. | ||||||
Leflunomide | 75706-12-6 | sc-202209 sc-202209A | 10 mg 50 mg | $20.00 $83.00 | 5 | |
Leflunomide metabolites inhibit AICAR transformylase, disrupting the enzyme's normal function in purine biosynthesis. | ||||||
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 indirectly inhibits AICAR transformylase by interfering with folate metabolism, which is crucial for purine synthesis. | ||||||
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, while primarily targeting bacterial enzymes, can indirectly affect AICAR transformylase through folate pathway interference. | ||||||
β-Pyrazofurin Trifluoroacetic Acid Salt | 30868-30-5 (free base) | sc-476809 | 1 mg | $480.00 | ||
Pyrazofurin inhibits AICAR transformylase by mimicking nucleotides, thereby disrupting the purine biosynthesis pathway. | ||||||
Azathioprine | 446-86-6 | sc-210853D sc-210853 sc-210853A sc-210853B sc-210853C | 500 mg 1 g 2 g 5 g 10 g | $203.00 $176.00 $349.00 $505.00 $704.00 | 1 | |
Azathioprine metabolites can inhibit AICAR transformylase, impacting purine nucleotide biosynthesis and accumulation. | ||||||
6-Mercaptopurine | 50-44-2 | sc-361087 sc-361087A | 50 mg 100 mg | $72.00 $104.00 | ||
6-Mercaptopurine, a purine analogue, inhibits AICAR transformylase by incorporating into the purine biosynthesis pathway and causing feedback inhibition. | ||||||
6-Thioguanine | 154-42-7 | sc-205587 sc-205587A | 250 mg 500 mg | $42.00 $54.00 | 3 | |
Thioguanine acts similarly to 6-mercaptopurine, inhibiting AICAR transformylase and interfering with purine nucleotide biosynthesis. | ||||||
Mizoribine | 50924-49-7 | sc-359617 sc-359617A | 10 mg 25 mg | $109.00 $228.00 | ||
MIZORIBINE inhibits AICAR transformylase by mimicking natural substrates of the enzyme, thereby affecting purine synthesis. | ||||||