1. MM-401

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (MM-401 TFA) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

MM-401 Chemical Structure

MM-401 Chemical Structure

CAS No. : 1442106-10-6

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Description

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[1].

IC50 & Target

Ki: < 1 nM (WDR5); IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 µM (MLL1)[1].

In Vitro

MM-401 maintains high binding affinity to WDR5 with a Ki value of < 1 nM and disrupts WDR5-MLL1 interaction with an IC50 value of 0.9 nM[1].
MM-401 is able to specifically inhibit MLL1 activity (IC50 value of 0.32µM) by blocking MLL1-WDR5 interaction and thus the complex assembly[1].
MM-401 (20 μM; 48 h) specifically inhibits MLL1-dependent H3K4 methylation in cells[1].
MM-401 induces similar changes in MLL-AF9 transcriptome as the MLL1 deletion[1].
MM-401 (10, 20, 40 μM; 48 h) specifically inhibits growth of MLL leukemia cells by inducing cell cycle arrest, apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: Murine MLL-AF9 and Hoxa9/Meis1 cells
Concentration: 0, 20, 40 μM
Incubation Time: 48 h
Result: Specifically induced apoptosis of MLL-AF9 cells.

Cell Cycle Analysis[1]

Cell Line: Murine MLL-AF9 and Hoxa9/Meis1 cells
Concentration: 10, 20, 40 μM
Incubation Time: 48 h
Result: Induced prominent G1/S arrest in MLL-AF9 cells in a concentration dependent manner.

RT-PCR[1]

Cell Line: MLL-AF9 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Significantly decreased H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10.
Molecular Weight

586.73

Formula

C29H46N8O5

CAS No.
SMILES

C[C@@](C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@@]1(C2=CC=CC=C2)[H])=O)CC)=O)=O)(NC(C(C)C)=O)CCCCNC1=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MM-401
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HY-19554
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