GSK429286A is a drug that is mostly used in the research environment to study protein kinases. This compound has been widely studied and has demonstrated to be an effective inhibitor of many diseases. GSK429286A belongs to the pyrido[3,2-d]pyrimidine family and has a molecular formula C19H17N5O2. The compound has a formula weight of 347.37 g/mol and a CAS No. of 864082-47-3.
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Health Benefits of GSK429286A GSK429286A has many potential health benefits, which are currently being studied in preclinical and clinical experiments. Researchers have found that GSK429286A has significant therapeutic activity against certain types of cancer, including ovarian, prostate, and breast cancer. GSK429286A works by inhibiting the PI3K/mTOR signaling pathway, which is overactive in many cancer types, allowing the cells to proliferate and survive better.
GSK429286A also has potential benefits as a treatment for neurodegenerative diseases. Studies have shown that autophagy inhibition leads to the accumulation of damaging cellular aggregates, which can cause cell death in neurodegenerative diseases. GSK429286A, an autophagy inhibitor, can potentially mitigate this effect, allowing normal cellular function and preventing cell death.
Potential Effects of GSK429286A GSK429286A inhibits autophagy by inhibiting PI3K/mTOR signaling, allowing researchers to study the mechanisms underlying autophagy in cellular metabolism. GSK429286A has demonstrated efficacy in preclinical models of human disease, such as cancer and neurodegenerative disease. There is potential for GSK429286A to be used in clinical settings for treatment of these diseases, but more research is required to fully understand its safety and efficacy.
Product Mechanism GSK429286A inhibits autophagy by targeting the PI3K/mTOR signaling pathway, which is overactive in many cancer types, allowing the cells to proliferate and survive better. GSK429286A selectively targets Class I PI3K isoforms by binding to the ATP-binding site of the kinase domain, blocking its active site. Consequently, this prevents phosphorylation of downstream targets, such as AKT, which results in downstream autophagy blockade. GSK429286A inhibits the growth and survival of cancer cells by blocking the autophagy response.
Safety of GSK429286A Researchers have conducted in vitro studies that evaluated GSK429286A's safety profile, with no significant risks or adverse effects noted. However, more clinical studies are needed to confirm its safety profile in humans as the majority of the studies to date have been preclinical.
Side Effects While GSK429286A is considered safe in preclinical studies, it could come with side effects when used in humans. These side effects could range from mild symptoms to life-threatening situations. Common side effects include gastrointestinal upset, dizziness, fatigue, headache, and fever. Rare side effects include seizures, cardiovascular dysfunction, and pancreatitis.
Dosing Information Recommended dosing information is not yet available for clinical use, but research on GSK429286A suggests that it should be used with caution and low doses should be given in a regulated manner. The dosage could be titrated based on individual patient response and drug tolerance.
Conclusion GSK429286A has shown great potential in targeting the PI3K/mTOR signaling pathway and mediating autophagy blockade, potentially making it a useful adjunct in the clinical management of various diseases, especially cancer and neurodegenerative disease. Its specificity and unique mechanism of action make it a promising candidate for drug therapy, although more studies are needed to fully understand its safety and efficacy before it can be used clinically.