MilliporeSigma™ Calbiochem™ HMTase Inhibitor IX, MM-102

Description

A cell-permeable peptidomimetic that prevents MLL1 (Mixed Lineage Leukemia 1) from complex assembling with WDR5 (Trp-Asp Repeat Domain 5), RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC₅₀

A cell-permeable peptidomimetic that prevents MLL1 (Mixed Lineage Leukemia 1) from complex assembling with WDR5 (Trp-Asp Repeat Domain 5), RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC₅₀ = 0.4nM). Shown to reduce HoxA9 and Meis-1 mRNA expression in myeloblasts derived from MLL1-AF9 -transduced murine bone marrow cells (50μM for 96 h) and preferentially inhibit the growth of MLL1-AF4-harboring MV4;11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI₅₀ in 7 days = 25μM) via apoptosis induction, while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI₅₀ in 7 days = 84μM).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Specifications

• Color: Light Beige
• Description: 95% by HPLC
• Target Proteins: WDR5
• Molecular Formula: C₃₅H₄₉F₂N₇O₄·CF₃CO₂H
• Solubility: DMSO
• Content And Storage: Hygroscopic, Protect from light
• Form: Powder
• Quantity: 10 mg