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MM-401 

Cat. No. M28443
MM-401  Structure
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Quality Control & Documentation
Biological Activity

MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 µM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia.

Chemical Information
Molecular Weight 586.73
Formula C29H46N8O5
CAS Number 1442106-10-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kebin Lu, et al. Front Oncol. The Histone H3 Lysine 4 Presenter WDR5 as an Oncogenic Protein and Novel Epigenetic Target in Cancer

[2] Hui Zhang, et al. Bio Protoc. Reprogram Murine Epiblast Stem Cells by Epigenetic Inhibitors

[3] Hacer Karatas, et al. J Med Chem. Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction

[4] Masoud Vedadi, et al. Protein Sci. Targeting human SET1/MLL family of proteins

[5] Fang Cao, et al. Mol Cell. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia

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  Catalog
Abmole Inhibitor Catalog




Keywords: MM-401  supplier, Histone Methyltransferase, inhibitors, activators


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