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In the realm of precision medicine and targeted cancer therapies, understanding the biochemical intricacies of key molecules is paramount. EPZ-5676, also known as Pinometostat, stands out as a critical research compound. It is a potent and selective inhibitor of DOT1L (Disruptor of telomeric silencing 1-like), a histone methyltransferase that plays a significant role in the epigenetic regulation of gene expression, particularly in the context of leukemia and other cancers.
Biochemical Properties and Mechanism of Action
EPZ-5676 is characterized by its molecular formula C30H42N8O3 and a molecular weight of approximately 562.71 g/mol. Its chemical structure enables it to act as a competitive inhibitor of S-adenosyl methionine (SAM) for the DOT1L enzyme. By binding to the SAM pocket, EPZ-5676 effectively blocks the methyltransferase activity of DOT1L, thereby preventing the methylation of histone H3 at lysine 79 (H3K79). This epigenetic mark is crucial for gene activation, and its aberrant regulation by DOT1L is a hallmark of certain leukemias, such as those with MLL rearrangements. The high specificity of EPZ-5676, with Ki values in the picomolar range for DOT1L and significantly lower activity against other methyltransferases, makes it a valuable tool for precise research applications.
In Vitro and In Vivo Efficacy
The biochemical profile of EPZ-5676 translates into significant biological activity. In vitro studies demonstrate its ability to potently inhibit the proliferation of MLL-rearranged leukemia cell lines, often with IC50 values in the low nanomolar range. Furthermore, it has been shown to promote apoptosis and downregulate key oncogenic target genes. In vivo studies have also yielded promising results, with EPZ-5676 demonstrating efficacy in reducing tumor burden and achieving complete regressions in animal models of leukemia. These findings underscore its potential as a therapeutic agent and highlight its importance as a research chemical.
Procuring EPZ-5676 for Your Research Needs
For scientists and researchers working in oncology, epigenetics, and pharmaceutical development, securing a reliable source of EPZ-5676 is essential. We, as a dedicated supplier and manufacturer in China, provide high-quality EPZ-5676 (CAS 1380288-87-8) that meets the rigorous demands of scientific research. Our commitment is to deliver compounds with verified purity and consistent performance. When you need to buy EPZ-5676, consider our comprehensive product offerings and expert support. We are equipped to handle inquiries for research quantities and bulk orders, ensuring that your supply chain for this critical DOT1L inhibitor remains robust. Contact us to learn more about pricing and availability, and let us be your trusted partner in advancing critical research.
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A: We don't have Minimum Order Quantity, exact quantity should be provided before quotation for us to calculate the exact cost.
A: We don't provide free samples due to lots of request and expensive international courier's cost, we can deduct the sample charge after commercial order placed.
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