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WDR5 WIN site inhibitor 16

Chemical Structure : WDR5 WIN site inhibitor 16

CAS No.: 2408842-51-1

WDR5 WIN site inhibitor 16

Catalog No.: PC-49506Not For Human Use, Lab Use Only.

WDR5 WIN site inhibitor 16 is a potent, selective inhibitor of WD repeat domain 5 (WDR5) WIN site with TR-FRET Kd of <0.02 nM, exhibits histone methyltransferase inhibition with IC50 of 2.2 nM.

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

    Biological Activity

    WDR5 WIN site inhibitor 16 is a potent, selective inhibitor of WD repeat domain 5 (WDR5) WIN site with TR-FRET Kd of <0.02 nM, exhibits histone methyltransferase inhibition with IC50 of 2.2 nM.
    WDR5 WIN site inhibitor 16 displaced WDR5 from chromatin and repressed mRNA expression of WDR5-bound genes.
    WDR5 WIN site inhibitor 16 (0.01-3 uM) induced p53 and p21 protein levels and apoptosis in MV4:11 cells.
    WDR5 WIN site inhibitor 16 displaced MYC from chromatin at WDR5-displaced genes.
    WDR5 WIN site inhibitor 16 exhibited potent anti-proliferative activity against MYC-driven cancer cells, including CHP-134 (neuroblastoma, wt p53, GI50=0.26 uM) and Ramos (Burkitt's lymphoma, mutant p53, GI50=0.49 uM).

    Physicochemical Properties

    M.Wt 514.60
    Formula C30H31FN4O3
    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-(3,5-Dimethoxybenzyl)-5-(4-fluoro-2-methylphenyl)-7-((2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one

    References

    1. Jianhua Tian, et al. J Med Chem. 2020 Jan 23;63(2):656-675.

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