Home Epigenetics Histone Methyltransferase inhibitor - MLL inhibitor MM-102 For research use only.

MM-102

Synonyms: HMTase Inhibitor IX

MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.This product may precipitate when dissolved in saline solution or PBS solution. It is recommended to prepare the stock solution in DMSO solution.

MM-102 Chemical Structure

MM-102 Chemical Structure

CAS No. 1417329-24-8

Purity & Quality Control

Batch: S726501 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]50 mg/mL]false Purity: 99.0%
99.0

MM-102 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Rosetta 2 (DE3) pLysS Function assay Inhibition of MLL1 binding to N-terminal His-tagged WRD5 23 deletion mutant (24 to 334 residues) (unknown origin) expressed in Escherichia coli Rosetta 2 (DE3) pLysS cells by fluorescence polarization assay, Ki = 0.001 μM. 29254892
Rosetta 2 (DE3) pLysS Function assay Inhibition of MLL1 binding to N-terminal His-tagged WRD5 23 deletion mutant (24 to 334 residues) (unknown origin) expressed in Escherichia coli Rosetta 2 (DE3) pLysS cells by fluorescence polarization assay, IC50 = 0.0024 μM. 29254892
Rosetta2-(DE3) pLysS Function assay 5 hrs Inhibition of C-terminal 5-FAM-WIN peptide binding to N-terminal His-tagged WDR5 (24 to 334 residues) (unknown origin) expressed in Rosetta2-(DE3) pLysS cells after 5 hrs by fluorescence polarization assay, IC50 = 0.0024 μM. 27720555
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay, IC50 = 20.7 μM. 27720555
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay, IC50 = 20.7 μM. 27598236
MV4-11 Antiproliferative assay 7 days Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay, IC50 = 25 μM. 27720555
MV4-11 Antiproliferative assay Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay, IC50 = 25 μM. 27598236
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay, IC50 = 37.8 μM. 27720555
K562 Growth inhibition assay 7 days Growth inhibition of human K562 cells after 7 days by MTS assay, IC50 = 37.8 μM. 27598236
MV4-11 Function assay 10 uM 7 days Inhibition of MLL1-WDR5 protein-protein interaction in human MV4-11 cells harboring MLL-AF4 fusion protein assessed as inhibition of MLL1 histone methyltransferase activity by measuring reduction in H3K4me2 level at 10 uM after 7 days by Western blot meth 27598236
Click to View More Cell Line Experimental Data

Biological Activity

Description MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.This product may precipitate when dissolved in saline solution or PBS solution. It is recommended to prepare the stock solution in DMSO solution.
Targets
WDR5 [1]
(Cell-free assay)
2.4 nM
In vitro
In vitro MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and Ki of < 1 nM. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins. [1]
Kinase Assay In Vitro Histone Methyltransferase (HMT) Assay
The HMT assay is performed in 50 mM HEPES pH 7.8, 100 mM NaCl, 1.0 mM EDTA, and 5% glycerol at 22 °C. Each reaction contains 1.5 μCi of the co-factor, 3H-S-adenosylmethionine. H3 10-residue peptide is used as the substrate at 50 μM. Compounds are added at concentrations ranging from 0.125 to 128 μM and incubated with the pre-assembled WDR5/RbBP5/ASH2L complex at a final concentration of 0.5 μM for each protein for 2–5 min. Reactions are initiated by addition of the MLL1 protein at a final concentration of 0.5 μM and allowed to proceed for 30 min before preparing scintillation counting. To count samples, reactions are spotted on separate squares of P81 filter paper and precipitated by submerging in freshly prepared 50 mM sodium bicarbonate buffer with pH 9.0. After washing and drying, samples are vortexed in Ultima Gold scintillation fluid and counted. As a negative control, assays are performed using 0.5 μM MLL1/WDR5/RbBP5/ASH2L complex assembled with the non-interacting mutant, WDR5D107A.
Cell Research Cell lines MV4;11, KOPN8, and K562 cells
Concentrations ~100 μM
Incubation Time 7 days
Method

MV4;11, KOPN8, and K562 cells are cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillin-streptomycin and incubated at 37 °C under 5% CO2. Cells are seeded into 12-well plates for suspension at a density of 5 × 105 per well (1 mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 for 7 days. The medium is changed every 2 days, and compounds are resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit is used following the manufacturer’s instruction. First, 100 μL of the assay reagent is added into each well, and the content is mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence is read on a microplate reader.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 23210835

Chemical Information & Solubility

Molecular Weight 669.8 Formula

C35H49F2N7O4
CAS No. 1417329-24-8 SDF Download MM-102 SDF
Smiles CCC(CC)(C(=O)NC(CCCN=C(N)N)C(=O)NC1(CCCC1)C(=O)NC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)NC(=O)C(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (149.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 50 mg/mL


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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