The intricate mechanisms of epigenetic regulation are increasingly becoming focal points in cancer research, offering new avenues for therapeutic intervention. At the forefront of this research is the enzyme DOT1L (Histone Lysine Methyltransferase DOT1L), a key player whose dysregulation is linked to aggressive hematological malignancies, notably MLL-rearranged leukemias. Pinometostat, identified by CAS 1380288-87-8 and often referred to as EPZ-5676, is a highly selective inhibitor designed to counteract DOT1L activity.

The scientific rationale behind Pinometostat's efficacy lies in its targeted inhibition of DOT1L. This enzyme is responsible for catalyzing the methylation of histone H3 at lysine 79 (H3K79 methylation). In MLL-rearranged leukemias, this process is dysregulated, leading to the activation of oncogenic genes that drive uncontrolled cell proliferation. Pinometostat's molecular design allows it to bind to the SAM binding pocket of DOT1L, effectively blocking its enzymatic function. This blockade leads to a reduction in oncogenic H3K79 methylation, thereby suppressing the expression of critical target genes such as HOXA9 and MEIS1, and ultimately promoting the differentiation or apoptosis of cancer cells.

For scientists and drug developers aiming to harness the power of epigenetic modulation, securing a reliable supply of high-quality Pinometostat is essential. Our company, a distinguished pharmaceutical intermediate manufacturer located in China, is committed to producing EPZ-5676 with exceptional purity and consistent quality. We serve the global research community, providing access to this critical compound that supports cutting-edge investigations into targeted cancer therapies.

Key scientific insights into Pinometostat (EPZ-5676):

  • Mechanism of Action: Potent and selective inhibition of DOT1L, crucial for understanding epigenetic control in cancer.
  • Therapeutic Target: Primarily used in research for MLL-rearranged leukemias, offering a targeted approach to treatment.
  • Preclinical Efficacy: Demonstrated ability to induce significant regression in leukemia xenograft models, validating its potential in vivo.
  • Selectivity Profile: High selectivity over other methyltransferases minimizes off-target effects, a vital consideration for drug development.
  • Availability for Research: We facilitate the purchase of Pinometostat (CAS 1380288-87-8) for laboratory use, ensuring researchers can acquire this vital tool.

We invite researchers interested in the science of epigenetics and targeted leukemia treatments to partner with us. Contact us for a quote on Pinometostat (EPZ-5676) and to learn more about our capabilities as a leading pharmaceutical intermediate supplier. Equip your research with the precise tools needed to drive innovation.