AKR1CL2 Inhibitors
AKR1CL2 inhibitors are a specialized class of chemical compounds designed to inhibit the activity of the AKR1CL2 enzyme, which is part of the aldo-keto reductase (AKR) superfamily. AKR1CL2, like other members of this enzyme family, catalyzes the reduction of aldehydes and ketones to their corresponding alcohols using NADPH as a cofactor. This reduction process is crucial for various metabolic pathways, including the detoxification of reactive aldehydes and the regulation of steroids, carbohydrates, and xenobiotics. AKR1CL2 inhibitors act by binding to the enzyme's active site, where they interfere with the binding of natural substrates or cofactor molecules, effectively blocking the catalytic reduction process. These inhibitors often mimic the structure of the enzyme's substrates or transition states, which allows them to competitively inhibit the enzyme by engaging key catalytic residues, such as those involved in NADPH binding and substrate positioning.
The structural design of AKR1CL2 inhibitors is heavily guided by detailed knowledge of the enzyme's three-dimensional conformation, typically obtained through structural biology techniques like X-ray crystallography or nuclear magnetic resonance (NMR) spectroscopy. These studies help reveal the specific features of the active site, such as hydrogen bonding networks, hydrophobic pockets, and key amino acid residues that are involved in substrate recognition and catalysis. Based on this information, inhibitors are designed with chemical groups like hydroxyls, carbonyls, or aromatic rings to interact effectively with these regions. Additionally, computational tools like molecular docking and molecular dynamics simulations are employed to predict how potential inhibitors will bind to AKR1CL2 and to optimize their binding strength and specificity. In some cases, allosteric inhibitors may also be developed to bind at sites outside the active site, inducing conformational changes that indirectly reduce the enzyme's activity. AKR1CL2 inhibitors are valuable tools for studying the enzyme's role in metabolic pathways and for gaining a deeper understanding of the biochemical mechanisms that govern the AKR enzyme family.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Flufenamic acid | 530-78-9 | sc-205699 sc-205699A sc-205699B sc-205699C | 10 g 50 g 100 g 250 g | $27.00 $79.00 $154.00 $309.00 | 1 | |
Flufenamic acid is a nonsteroidal anti-inflammatory drug that inhibits chloride channels. By targeting these channels, the cellular environment is altered, leading to modulation of the redox state and impacting the activity of AKR1CL2, which is sensitive to redox changes. | ||||||
Indomethacin | 53-86-1 | sc-200503 sc-200503A | 1 g 5 g | $29.00 $38.00 | 18 | |
Indomethacin, another NSAID, inhibits cyclooxygenase enzymes (COX-1 and COX-2). By altering prostaglandin synthesis, it indirectly affects the cellular redox state, which can inhibit AKR1CL2 activity due to its redox-sensitive nature. | ||||||
Mefenamic acid | 61-68-7 | sc-205380 sc-205380A | 25 g 100 g | $106.00 $208.00 | 6 | |
Mefenamic acid is a member of the fenamate group of NSAIDs. It inhibits the synthesis of inflammatory mediators. Its action also alters the cellular redox balance, which can indirectly inhibit the activity of redox-sensitive proteins like AKR1CL2. | ||||||
Sulindac | 38194-50-2 | sc-202823 sc-202823A sc-202823B | 1 g 5 g 10 g | $32.00 $86.00 $150.00 | 3 | |
Sulindac is a sulfoxide that gets reduced in the body to an active sulfide form. This reduction process within cells can influence the cellular redox status, thereby potentially inhibiting redox-sensitive proteins such as AKR1CL2. | ||||||
Omeprazole | 73590-58-6 | sc-202265 | 50 mg | $67.00 | 4 | |
Omeprazole is a proton pump inhibitor that can alter intracellular pH. This alteration could affect the enzymatic activity of proteins that are pH-sensitive, potentially including AKR1CL2 if its activity is pH-dependent. | ||||||
Allopurinol | 315-30-0 | sc-207272 | 25 g | $131.00 | ||
Allopurinol inhibits xanthine oxidase, leading to lower production of uric acid and reactive oxygen species (ROS). Reduced ROS levels can influence the redox balance, potentially impacting the activity of redox-sensitive enzymes like AKR1CL2. | ||||||
Methotrexate | 59-05-2 | sc-3507 sc-3507A | 100 mg 500 mg | $94.00 $213.00 | 33 | |
Methotrexate acts as a dihydrofolate reductase inhibitor, influencing nucleotide biosynthesis and cellular proliferation. This can indirectly affect the redox state of the cell, potentially modulating the activity of AKR1CL2. | ||||||
Auranofin | 34031-32-8 | sc-202476 sc-202476A sc-202476B | 25 mg 100 mg 2 g | $153.00 $214.00 $4000.00 | 39 | |
Auranofin is a gold-containing compound that inhibits thioredoxin reductase, leading to changes in cellular redox state. Inhibition of this enzyme can lead to the indirect inhibition of redox-sensitive proteins such as AKR1CL2. | ||||||
Disulfiram | 97-77-8 | sc-205654 sc-205654A | 50 g 100 g | $53.00 $89.00 | 7 | |
Disulfiram inhibits aldehyde dehydrogenase, affecting acetaldehyde metabolism and leading to altered redox states within the cell. This can impact redox-dependent enzymes like AKR1CL2. | ||||||
Vitamin K3 | 58-27-5 | sc-205990B sc-205990 sc-205990A sc-205990C sc-205990D | 5 g 10 g 25 g 100 g 500 g | $26.00 $36.00 $47.00 $136.00 $455.00 | 3 | |
Menadione is a synthetic compound that can undergo redox cycling, producing ROS in cells. The resulting alteration of the redox environment can modulate the activity of redox-sensitive proteins like AKR1CL2. | ||||||