MM-401 | CAS No. 1442106-10-6

Description

Product Description

MM-401 (CAS 1442106-10-6) is a small-molecule inhibitor specifically designed to disrupt the MLL1–WDR5 protein-protein interaction, a crucial step in the regulation of histone H3 lysine 4 (H3K4) methylation. This epigenetic mark plays a central role in regulating gene expression, and its dysregulation has been strongly linked to mixed lineage leukemia (MLL) and other cancers.

Background on MLL1 and Epigenetic Regulation

• MLL1 (Mixed-Lineage Leukemia 1) is a histone methyltransferase that catalyzes H3K4 methylation, an epigenetic modification associated with transcriptional activation.

• MLL1 functions within a multi-protein complex requiring co-factors such as WDR5, RbBP5, and ASH2L.

• Dysregulation of MLL1 activity leads to aberrant transcription of genes involved in hematopoietic differentiation and oncogenesis.

Role of MM-401 in Research

1. Leukemia Studies

   • MLL-rearranged leukemias are aggressive hematological malignancies with poor prognosis.

   • MM-401 selectively inhibits leukemic cell growth by targeting MLL1-WDR5 interactions.

   • Promotes cell cycle arrest, apoptosis, and differentiation of leukemic blasts.

2. Epigenetic Mechanism Exploration

   • Serves as a model compound for understanding histone methyltransferase biology.

   • Helps delineate the role of H3K4 methylation in transcription regulation.

3. Drug Discovery Tool

   • Acts as a chemical probe to validate the therapeutic potential of disrupting MLL complexes.

   • Guides development of next-generation MLL1 inhibitors.

4. Free Form vs. Salt Form (MM-401 TFA)

   • Both demonstrate equivalent biological activity at equimolar concentrations.

   • TFA salt form provides enhanced water solubility and chemical stability, making it more suitable for biological assays.

Product Specifications

Notes

• Supplied in both free and TFA salt forms.

• Endotoxin-free.

• For research use only.

Mechanism of Action

MM-401 functions by selectively blocking the interaction of MLL1 with WDR5, thereby inhibiting MLL1-mediated methylation of histone H3 at lysine 4 (H3K4).

1. Disruption of MLL1-WDR5 Interaction

   • WDR5 is essential for stabilizing MLL1 complex formation.

   • MM-401 binds to the WDR5 interaction site, preventing recruitment of MLL1.

2. Inhibition of H3K4 Methylation

   • Loss of MLL1 activity reduces H3K4 trimethylation.

   • Leads to downregulation of genes critical for leukemogenesis, such as HOXA9 and MEIS1.

3. Cell Cycle Arrest

   • Inhibition of transcriptional programs controlled by MLL1 halts proliferation.

   • Leukemic cells undergo G0/G1 arrest.

4. Induction of Apoptosis

   • Triggered by downregulation of survival genes.

   • Leads to caspase activation and programmed cell death.

5. Differentiation of Leukemic Cells

   • By relieving epigenetic blocks, MM-401 promotes terminal differentiation.

6. Epigenetic Selectivity

   • Unlike global histone methyltransferase inhibitors, MM-401 is highly selective for the MLL1-WDR5 interaction.

   • Minimizes off-target effects and provides a precise research tool.

     

Side Effects

Research Observations

• Demonstrates high selectivity for MLL1-WDR5 with minimal off-target inhibition.

• Reduces leukemic cell viability while sparing most normal hematopoietic cells.

Potential Research Risks

• Prolonged exposure may alter gene expression landscapes in non-leukemic cells.

• Possible cytotoxicity at high concentrations.

• Stability of the free form is lower compared to TFA salt.

Laboratory Safety Notes

• For laboratory research only.

• Handle under sterile conditions.

• Store in recommended conditions to preserve activity.

Disclaimer

This product is intended for research purposes only. MM-401 is not approved for clinical or diagnostic use in humans.

Keywords

MM-401, CAS 1442106-10-6, MLL1 inhibitor, WDR5-MLL1 interaction blocker, H3K4 methyltransferase inhibitor, MM-401 TFA, leukemia research compound, epigenetic inhibitor.china low price supplier 

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