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500649 HMTase Inhibitor IX, MM-102 - Calbiochem

500649
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Overview

Key Spec Table

Empirical Formula
C₃₅H₄₉F₂N₇O₄ · CF₃CO₂H

Products

Catalogue NumberPackaging Qty/Pack
5.00649.0001 Sklená flaša 10 mg
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
Biological Information
Primary TargetWDR5
Primary Target K<sub>i</sub>1 nM)
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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
Global Trade Item Number
Catalogue Number GTIN
5.00649.0001 04055977245035