FMO2 Inhibitors
Chemical inhibitors of FMO2 can engage with the enzyme in a variety of ways to impede its normal metabolic functioning. Methylene blue, for instance, operates by diminishing the levels of nitric oxide, a known modulator of FMO2, thereby leading to a decrease in FMO2 activity. Substrate competition is a common inhibitory mechanism, as seen with Chlorzoxazone, which can saturate the active site of FMO2 and prevent the metabolism of other substrates. Similarly, Indole-3-carbinol and Itopride may bind to the enzyme's active site and obstruct access to endogenous substrates, leading to reduced enzymatic action.
Mechanism-based or suicide inhibition is another route through which FMO2 can be inhibited. Compounds like Benzamidoxime and Tetrahydrothiophene undergo bioactivation by FMO2, after which they become reactive and covalently bind to the enzyme, resulting in irreversible inhibition. Methimazole acts in a similar fashion by binding covalently to the active site, leading to a lasting decrease in FMO2 activity. Phenylthiourea is known to impede several xenobiotic-metabolizing enzymes, including FMO2, by directly blocking the active site. Ethionamide, a prodrug, requires activation by FMO2 but can also serve as a mechanism-based inhibitor as its bioactivated form inactivates the enzyme. Lastly, Ticlopidine hampers FMO2 function through active site binding, which effectively inhibits the enzyme by preventing the metabolism of other substrates.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Methylene blue | 61-73-4 | sc-215381B sc-215381 sc-215381A | 25 g 100 g 500 g | $43.00 $104.00 $328.00 | 3 | |
Methylene blue is an inhibitor of nitric oxide synthase, which can reduce the levels of nitric oxide, a known modulator of FMO2 activity. Lower nitric oxide levels can lead to decreased FMO2 function as the protein is sensitive to nitric oxide levels. | ||||||
Chlorzoxazone | 95-25-0 | sc-211078 | 10 mg | $62.00 | ||
Chlorzoxazone is a substrate for FMO2 and at high concentrations can act as an inhibitor. It competes for the active site of FMO2, thereby inhibiting its metabolic activity. | ||||||
Benzamide oxime | 613-92-3 | sc-268545 | 1 g | $171.00 | ||
Benzamidoxime can inhibit FMO2 by acting as a mechanism-based inhibitor, where it is bioactivated by FMO2 and subsequently binds irreversibly to the active site, leading to a decrease in FMO2 activity. | ||||||
Tranylcypromine | 13492-01-8 | sc-200572 sc-200572A | 1 g 5 g | $175.00 $599.00 | 5 | |
Tranylcypromine, a monoamine oxidase inhibitor, can also inhibit FMO2 by acting as a substrate that competes with other substrates for the active site, leading to decreased FMO2 activity. | ||||||
Indole-3-carbinol | 700-06-1 | sc-202662 sc-202662A sc-202662B sc-202662C sc-202662D | 1 g 5 g 100 g 250 g 1 kg | $39.00 $61.00 $146.00 $312.00 $1032.00 | 5 | |
Indole-3-carbinol is metabolized by FMO2 and can inhibit the enzyme by competing with other substrates for binding at the active site, resulting in decreased enzymatic activity. | ||||||
Methimazole | 60-56-0 | sc-205747 sc-205747A | 10 g 25 g | $70.00 $112.00 | 4 | |
Methimazole acts as a mechanism-based inhibitor of FMO2. It is bioactivated by the enzyme and subsequently binds covalently to the active site, leading to a functional inhibition of FMO2. | ||||||
Tetrahydrothiophene | 110-01-0 | sc-258232 | 1 g | $20.00 | ||
Tetrahydrothiophene is metabolized by FMO2 and can act as a suicide inhibitor. Upon metabolism by FMO2, it becomes a reactive metabolite that irreversibly binds to and inhibits the enzyme. | ||||||
N-Phenylthiourea | 103-85-5 | sc-236086 | 100 g | $319.00 | ||
Phenylthiourea is known to inhibit various enzymes involved in xenobiotic metabolism, including FMO2. It can bind to the active site of FMO2, blocking access to other substrates and leading to an inhibition of its metabolic function. | ||||||
Ethionamide | 536-33-4 | sc-211429 | 5 g | $250.00 | ||
Ethionamide is a prodrug that requires activation by FMO2. It can act as a mechanism-based inhibitor as the bioactivated form reacts with the enzyme, reducing FMO2 activity. | ||||||
Ticlopidine Hydrochloride | 53885-35-1 | sc-205861 sc-205861A | 1 g 5 g | $32.00 $99.00 | 2 | |
Ticlopidine is a known inhibitor of various drug-metabolizing enzymes. It inhibits FMO2 by binding to the active site, which prevents the metabolism of other substrates by FMO2 and leads to its functional inhibition. | ||||||