MM-102

SKU: orb1300860

Description

MM-102 is a potent small molecule inhibitor of the WDR5-MLL interaction with sub-nanomolar affinity. It selectively impedes proliferation and triggers apoptosis in MLL-rearranged leukemia cells in vitro, serving as a critical chemical probe for epigenetic and cancer research.

Research Area

Cell Biology, Epigenetics & Chromatin, Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1417329-24-8
• MW: 669.8
• Purity: 99.99% (May vary between batches)
• Formula: C₃₅H₄₉F₂N₇O₄
• SMILES: C(NC(C1=CC=C(F)C=C1)C2=CC=C(F)C=C2)(=O)C3(NC([C@@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(=N)N)=O)CCCC3
• Target: Histone Methyltransferase,TNF,NF-κB,Apoptosis,Interleukin
• Solubility: DMSO:140 mg/mL (209.02 mM);H2O:92 mg/mL (137.35 mM);Ethanol:93 mg/mL (138.85 mM)

Bioactivity

• Target IC50:
  MLL1:0.4 μM
• In Vitro:
  METHODS: MLL1-AF9 transduced mouse cells were treated with MM-102 (HMTase Inhibitor IX) (25, 50 μM), and gene expression analysis was performed using quantitative RT-PCR (QRT-PCR). RESULTS MM-102 reduced HoxA9 mRNA expression in a dose-dependent manner. MM-102 significantly decreased Meis-1 expression at 50 μM. MM-102 did not affect the expression of the housekeeping gene GAPDH. METHODS: Cells were pretreated with 20 μM MM-102 (20 μM, 20 hours) for 24 hours and then incubated with 500 μM SNP. Cell apoptosis activity was evaluated approximately 24 hours later. RESULTS SNP significantly stimulated chondrocyte apoptosis, while cells pretreated with MM-102 alleviated SNP-stimulated chondrocyte apoptosis. MM-102 pretreatment effectively rescued the negative effects of FSS on chondrocytes, which may lay the foundation for epigenetic-based OA treatment.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, MM 102, MM102, MM-102, MLL1, Inhibitor, Histone Methyltransferase, HistoneMethyltransferase, HMTase Inhibitor IX

Compound Identifiers

PubChem CID

54766613