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500649 HMTase Inhibitor IX, MM-102 - Calbiochem

500649
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₅H₄₉F₂N₇O₄ · CF₃CO₂H

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      Description
      OverviewA 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 = 0.4 nM). Shown to reduce HoxA9 and Meis-1 mRNA expression in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells (50 µM 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 = 25 µM) via apoptosis induction, while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84 µM).

      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.
      Catalogue Number500649
      Brand Family Calbiochem®
      Synonyms(S)-N-(bis(4-Fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide, TFA, Histone Methyltransferase Inhibitor IX, MM102
      References
      ReferencesKaratas, H., et al. 2013. J. Am. Chem. Soc. 135, 669.
      Product Information
      FormLight beige powder
      Hill FormulaC₃₅H₄₉F₂N₇O₄ · CF₃CO₂H
      Chemical formulaC₃₅H₄₉F₂N₇O₄ · CF₃CO₂H
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetWDR5
      Primary Target K<sub>i</sub>1 nM)
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      HMTase Inhibitor IX, MM-102 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Karatas, H., et al. 2013. J. Am. Chem. Soc. 135, 669.

      Technical Info

      Title
      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision26-July-2013 JSW
      Synonyms(S)-N-(bis(4-Fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide, TFA, Histone Methyltransferase Inhibitor IX, MM102
      DescriptionA cell-permeable peptidomimetic that competes against MLL1 (Mixed Lineage Leukemia 1) minimum essential WIN (WDR5 INteracting) motif (-Ala3764-Arg-Ala3766-) for WDR5 (Trp-Asp Repeat Domain 5) binding (IC50/Ki = 2.5 nM/<1 nM and 540 nM/120 nM, respectively), effectively preventing MLL1 from complex assembling with WDR5, RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC50 = 0.4 nM). Shown to reduce HoxA9 and Meis-1 mRNA expression (by 76% and 36%, respectively, after 96 h 50 µM MM-102 treatment) in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells and preferentially inhibit the growth of MLL1-AF4-harboring MV4;11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25 µM) via apoptosis induction (by >75% in 4 days in MV4:11 cultures; 50 µM MM-102), while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84 µM; >90 live cells after 4-day 50 µM MM-102 treatment).
      FormLight beige powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₅H₄₉F₂N₇O₄ · CF₃CO₂H
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage -20°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKaratas, H., et al. 2013. J. Am. Chem. Soc. 135, 669.