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MGP-39

Chemical Structure : MGP-39

CAS No.: 3124031-73-5

MGP-39 (MELK PROTAC MGP-39)

Catalog No.: PC-22852Not For Human Use, Lab Use Only.

MGP-39 is a first-in-class PROTAC degrader targeting maternal embryonic leucine zipper kinase (MELK), induced potent and rapid degradation of MELK in Burkitt lymphoma cell (Dmax=91.6%), and IC50 of 1.8 uM for RAMOS cell line.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    MGP-39 is a first-in-class PROTAC degrader targeting maternal embryonic leucine zipper kinase (MELK), induced potent and rapid degradation of MELK in Burkitt lymphoma cell (Dmax=91.6%), and IC50 of 1.8 uM for RAMOS cell line.
    MGP-39 potently inhibits the phosphorylation of mTOR in accordance with MELK downregulation.
    MGP-39 exhibits the lower cytotoxicity against MDA-MB-231 cells compared to MELK inhibitors JNJ-47117096/MELK-8a.
    MGP-39 induces cell cycle arrest and apoptosis in BL cells.

    Physicochemical Properties

    M.Wt 845.96
    Formula C44H51N11O7
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    2-(2,6-dioxopiperidin-3-yl)-5-((2-(2-(2-(4-((4-(4-(4-(3-isobutoxypyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethyl)amino)isoindoline-1,3-dione

    References

    1. Yonghui Sun, et al. RSC Med Chem. 2024 Jun 4;15(7):2351-2356.

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