CPI203 (CAS: 1446144-04-2) is a small molecule inhibitor that has been studied for its potential use in cancer treatment. It was first identified by researchers at Cancer Research UK and has since undergone multiple studies to investigate its mechanism of action, safety profile, and efficacy. In this article, we will explore the chemical properties, health benefits, potential effects, product mechanism, safety, side effects, dosing information of CPI203 and provide a conclusion about its current status as a therapeutic agent.
Chemical Properties: CPI203 is a synthetic small molecule with the chemical name N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)-2-[(4-methylpiperazin-1-yl)methyl]acetamide. Its molecular formula is C21H29N3O2S, and its molecular weight is 391.54 g/mol. It is a white to off-white powder that is soluble in DMSO and ethanol.
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Health Benefits: CPI203 has been studied primarily for its potential use in cancer treatment. Studies have shown that it inhibits the growth of various types of cancer cells, including breast, prostate, and lung cancer cells. CPI203 works by targeting a protein called histone deacetylase 8 (HDAC8), which plays an important role in regulating gene expression. By inhibiting HDAC8, CPI203 can induce apoptosis and affect transcriptional regulation, leading to anti-tumor effects.
Potential Effects: In addition to its potential use in cancer treatment, CPI203 has also shown promise in treating other diseases related to epigenetics, such as Huntington's disease and spinal muscular atrophy. Studies have shown that CPI203 can increase the levels of SMN protein, which is involved in the development and maintenance of motor neurons. This suggests that CPI203 could potentially be used to treat neurodegenerative diseases.
Product Mechanism: CPI203 exerts its effects by selectively inhibiting the activity of HDAC8, which is a member of the histone deacetylase family of enzymes. HDACs play an important role in the regulation of gene expression by removing acetyl groups from histones, which affects chromatin structure and gene expression. By inhibiting HDAC8, CPI203 can affect transcriptional regulation, leading to anti-tumor effects and the induction of apoptosis.
Safety: The safety profile of CPI203 in humans remains unclear, as it is still in the preclinical stage of development. Further research is needed to evaluate its toxicity and potential side effects.
Side Effects: The potential side effects of CPI203 are currently unknown. However, some studies have suggested that HDAC inhibitors could affect the expression of genes involved in neuronal development and function, which could lead to cognitive impairment. Further studies are needed to evaluate the long-term safety of this compound.
Dosing Information: The optimal dose of CPI203 has not yet been established. In preclinical studies, doses ranging from 0.1 to 50 mg/kg have been used. More research is needed to determine the appropriate dose range for clinical use.
Conclusion: CPI203 is a promising small molecule inhibitor with potential applications in cancer treatment and other diseases related to epigenetics. Its ability to selectively inhibit the activity of HDAC8 makes it an attractive candidate for further study. However, its safety profile in humans needs to be established before it can be recommended for clinical use. With further research, CPI203 could potentially become an important tool in the fight against cancer and other epigenetic-related diseases