RCL Inhibitors
Chemical inhibitors of recombinant urate oxidase (RCL) function primarily by modulating the availability of its substrates in the purine degradation pathway. Allopurinol and its active metabolite, oxipurinol, as well as febuxostat and topiroxostat, target the enzyme xanthine oxidase. By inhibiting this enzyme, these compounds reduce the production of xanthine and uric acid, thus limiting the availability of substrates for RCL to act upon. This results in a functional inhibition of RCL's activity, as the enzyme has fewer molecules to interact with. Sulfinpyrazone and probenecid, while functioning differently by affecting the reabsorption and excretion of urate, also contribute to the limitation of substrate availability for RCL, by altering uric acid levels in the body.
Methotrexate, by inhibiting dihydrofolate reductase, leads to reduced levels of tetrahydrofolate, which is necessary for the synthesis of purine nucleotides. With fewer purine bases being synthesized, RCL finds its function inhibited due to diminished substrate availability. Similarly, azathioprine and 6-mercaptopurine interfere with purine metabolism through their metabolites, which again leads to a scarcity of substrates for RCL. Tisopurine, another xanthine oxidase inhibitor, reduces the production of metabolites within the purine degradation pathway, resulting in a functional inhibition of RCL. Pegloticase and rasburicase, both uric acid-specific enzymes, directly catalyze the conversion of uric acid to allantoin, effectively depleting the substrate RCL would process, thus inhibiting its function. Overall, these chemical inhibitors utilize various strategies to reduce the concentration of purine derivatives, which are necessary for RCL activity, thereby inhibiting the protein's function.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Allopurinol | 315-30-0 | sc-207272 | 25 g | $128.00 | ||
Allopurinol inhibits xanthine oxidase, an enzyme upstream of RCL's activity in the purine degradation pathway. By reducing the formation of xanthine and uric acid, allopurinol can decrease the substrate availability for RCL, leading to its functional inhibition. | ||||||
Methotrexate | 59-05-2 | sc-3507 sc-3507A | 100 mg 500 mg | $92.00 $209.00 | 33 | |
Methotrexate competitively inhibits dihydrofolate reductase (DHFR), which is necessary for the synthesis of tetrahydrofolate. As tetrahydrofolate is required for the synthesis of purine nucleotides, methotrexate's inhibition of DHFR can result in reduced levels of purine bases, thus inhibiting RCL by limiting its substrate availability. | ||||||
6-Mercaptopurine | 50-44-2 | sc-361087 sc-361087A | 50 mg 100 mg | $71.00 $102.00 | ||
6-Mercaptopurine is metabolized into thioguanine nucleotides which interfere with purine metabolism. This inhibition can result in the functional inhibition of RCL by reducing the pool of purine derivatives that RCL may act upon. | ||||||
Azathioprine | 446-86-6 | sc-210853D sc-210853 sc-210853A sc-210853B sc-210853C | 500 mg 1 g 2 g 5 g 10 g | $199.00 $173.00 $342.00 $495.00 $690.00 | 1 | |
Azathioprine is converted in vivo to 6-mercaptopurine. By acting through the same mechanism as 6-mercaptopurine, azathioprine can decrease the availability of purine bases, thus inhibiting the function of RCL by reducing its substrate pool. | ||||||
Febuxostat | 144060-53-7 | sc-207680 | 10 mg | $168.00 | 3 | |
Febuxostat selectively inhibits xanthine oxidase, leading to decreased production of uric acid. Since RCL is involved in the purine degradation pathway, the inhibition of upstream reactions by febuxostat can lead to a functional inhibition of RCL by lowering the availability of its substrates. | ||||||
(±)-Sulfinpyrazone | 57-96-5 | sc-202822 sc-202822A | 1 g 5 g | $39.00 $92.00 | 2 | |
Sulfinpyrazone is a uricosuric agent that can also inhibit the reabsorption of urate. By influencing the purine degradation pathway and potentially altering the concentration of substrates or products that RCL would act upon, sulfinpyrazone can inhibit the function of RCL. | ||||||
Probenecid | 57-66-9 | sc-202773 sc-202773A sc-202773B sc-202773C | 1 g 5 g 25 g 100 g | $27.00 $38.00 $98.00 $272.00 | 28 | |
Probenecid inhibits the reabsorption of uric acid in the kidneys and increases its excretion. By altering uric acid levels, probenecid can affect the purine degradation pathway, thereby inhibiting RCL through a reduction in substrate availability. | ||||||
Oxipurinol | 2465-59-0 | sc-208138 sc-208138A | 100 mg 500 mg | $218.00 $744.00 | 1 | |
Oxipurinol, the active metabolite of allopurinol, inhibits xanthine oxidase, which can functionally inhibit RCL by reducing the generation of its substrates in the purine degradation pathway. | ||||||