The field of epigenetics has revolutionized our understanding of diseases like cancer, providing novel targets for therapeutic intervention. Among these targets, DOT1L (Histone Lysine Methyltransferase DOT1L) has emerged as particularly significant, especially in the context of MLL-rearranged leukemias. Pinometostat, also known as EPZ-5676 (CAS 1380288-87-8), is a highly selective inhibitor of DOT1L, making it a crucial compound for researchers investigating these complex diseases.

Pinometostat's chemical structure, a complex organic molecule, is designed to bind specifically to the SAM (S-adenosyl methionine) binding pocket of DOT1L. This precise interaction disrupts the enzyme's activity, leading to the reversal of aberrant H3K79 methylation—a hallmark of MLL-fusion leukemia. The compound exhibits remarkable selectivity, being thousands of times more potent against DOT1L than other methyltransferases, which is critical for minimizing off-target effects and maximizing therapeutic efficacy.

For research institutions and pharmaceutical developers, obtaining high-quality Pinometostat is essential for advancing studies into its mechanism of action and therapeutic applications. As a dedicated manufacturer of pharmaceutical intermediates, we pride ourselves on producing EPZ-5676 that meets rigorous purity standards. Our commitment as a supplier in China ensures that you can reliably purchase this compound for your experiments, whether they are focused on cellular assays, in vivo models, or early-stage drug development.

Key aspects of Pinometostat (EPZ-5676) for researchers include:

  • Biological Activity: Its potent and selective inhibition of DOT1L is the cornerstone of its value. The low IC50 value (0.8 nM) for DOT1L inhibition highlights its strength as a research tool.
  • Therapeutic Relevance: Studies have shown that Pinometostat can induce complete and sustained regression in animal models of MLL-rearranged leukemia, demonstrating its potential as a clinical candidate. It effectively reduces the expression of MLL-fusion target genes like HOXA9 and MEIS1.
  • Chemical Properties: Understanding its form (typically a white to light yellow solid), solubility (e.g., in DMSO), and molecular weight (562.71 g/mol) is vital for laboratory handling and experimental design. We provide comprehensive product data upon request.
  • Manufacturer and Supplier Information: When you need to buy Pinometostat, choosing a manufacturer in China that emphasizes quality and reliability is crucial. We are committed to being your trusted source for this vital pharmaceutical intermediate.

We encourage researchers interested in epigenetic modifications and targeted cancer therapies to explore the capabilities of Pinometostat. Contact us today for a quote on EPZ-5676 (CAS 1380288-87-8) and discover how our high-quality pharmaceutical intermediates can support your groundbreaking research.