MM-401

Research use only, not for human use.

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM.

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM; represents over 3 and 700 folds more potency relative to MM-101 (IC50=2.9 nM) and the WDR5-interacting motif in MLL1 (WIN, IC50=750 nM); specifically blocks proliferation of MLL cells and induces changes in gene expression similar to those of MLL1 deletion; reprograms mouse epiblast stem cells (EpiSCs) to naive pluripotency.

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.MM-401 is able to specifically inhibit MLL1 activity (IC50 value of 0.32μM) by blocking MLL1-WDR5 interaction and thus the complex assembly.MM-401 (20 μM; 48 h) specifically inhibits MLL1-dependent H3K4 methylation in cells.MM-401 induces similar changes in MLL-AF9 transcriptome as the MLL1 deletion.MM-401 (10, 20, 40 μM; 48 h) specifically inhibits growth of MLL leukemia cells by inducing cell cycle arrest, apoptosis.Apoptosis Analysis 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 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 Cell Line:MLL-AF9 cellsConcentration:20 μM Incubation Time:48 h Result:Significantly decreased H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10.

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MM 401 | MM401

Chromatin/Epigenetic

HMTase

HMTase

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1442106-10-6

586.726

C29H46N8O5

>98% (HPLC)

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CC(C)C(N[C@@]1(C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC)C(N[C@H](C2=CC=CC=C2)C(NCCCC1)=O)=O)=O)=O)=O

N-((3R,6S,9S,12R)-6-ethyl-9-(3-guanidinopropyl)-12-methyl-2,5,8,11-tetraoxo-3-phenyl-1,4,7,10-tetraazacyclohexadecan-12-yl)isobutyramide

(-20℃)

With Ice Pack

≥ 2 years