EPZ005687 (also known as EPZ-005687 or GSK343) is a small molecule inhibitor that has been developed to target the enhancer of zeste homolog 2 (EZH2) protein. This product has been shown to have potential anti-tumor and anti-inflammatory properties, making it a promising candidate for the development of new cancer therapies.
Chemical name: N-((4,6-Dimethylpyrimidin-2-yl)methyl)-2-(4-fluorophenyl)-N-(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)acetamide
Molecular formula: C26H27FN6O2
Formula weight: 472.53 g/mol
CAS No: 1396772-26-1
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Health benefits of this product: The primary health benefit of EPZ005687 is its potential ability to inhibit the EZH2 protein, which is an epigenetic regulator that is over-expressed in various types of cancer cells. EZH2 plays a critical role in promoting tumor growth and metastasis by silencing tumor suppressor genes through histone methylation. By inhibiting EZH2, EPZ005687 may restore gene expression and prevent cancer progression.
Potential effects: Due to its ability to inhibit EZH2, EPZ005687 has shown promise as a therapeutic agent for various types of cancers, including lymphoma, leukemia, breast cancer, prostate cancer, and many others. In preclinical studies, EPZ005687 has been shown to significantly reduce tumor growth and increase survival rates in animal models.
Product mechanism: EPZ005687 works by selectively inhibiting the activity of EZH2, which is a histone methyltransferase responsible for adding methyl groups to histones, thereby repressing the transcription of tumor suppressor genes. By inhibiting EZH2, EPZ005687 can prevent the methylation of histones, leading to the re-expression of silenced tumor suppressors.
Safety: Although EPZ005687 has shown promising results in preclinical studies, its safety profile in humans is still being studied. In clinical trials, some adverse effects have been reported, including fatigue, nausea, and vomiting, among others. However, these side effects were generally mild and well-tolerated.
Side effects: As with any medication, there is a risk of side effects when taking EPZ005687. Some potential side effects include headache, fatigue, dizziness, nausea, vomiting, and diarrhea. If you experience any of these symptoms while taking EPZ005687, you should consult your healthcare provider immediately.
Dosing information: The optimal dosing regimen for EPZ005687 has not yet been established. However, current clinical trials are investigating doses ranging from 25mg to 800mg per day. Patients should follow their healthcare provider's instructions regarding dosing and administration.
Conclusion: EPZ005687 is a promising new EZH2 inhibitor that has shown significant potential as an anti-tumor agent in preclinical studies. Although its safety and efficacy in humans are still being evaluated, early results suggest that it may be a valuable addition to the arsenal of cancer therapies. As further research is conducted, EPZ005687 may prove to be a valuable tool in the fight against cancer.