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MM-102

Catalog No. T6333 CAS 1417329-24-8

Synonyms: MM102, HMTase Inhibitor IX

MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

MM-102, CAS 1417329-24-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 107.00
10 mg	In stock	$ 177.00
25 mg	In stock	$ 370.00
50 mg	In stock	$ 572.00
100 mg	In stock	$ 818.00
1 mL * 10 mM (in DMSO)	In stock	$ 158.00

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Purity: 99.08%

Purity: 98.77%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
Targets&IC50	MLL1:0.4 μM
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	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. (Only for Reference)

Synonyms	MM102, HMTase Inhibitor IX
Molecular Weight	669.8
Formula	C35H49F2N7O4
CAS No.	1417329-24-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (138.8 mM)

H2O: 92 mg/mL (137.4 mM)

Ethanol: 93 mg/mL (138.8 mM)

References and Literature

1. Karatas H, et al. J Am Chem Soc. 2013, 135(2), 669-682.

Citations

1. Wang S, Lin Y, Gao L, et al. PPAR-γ integrates obesity and adipocyte clock through epigenetic regulation of Bmal1. Theranostics. 2022, 12(4): 1589.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library Bioactive Compound Library Bioactive Compounds Library Max PPI Inhibitor Library Epigenetics Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MM-102 1417329-24-8 Chromatin/Epigenetic Histone Methyltransferase MM102 HMTase Inhibitor IX MM 102 Inhibitor inhibit inhibitor

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