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SKLB-0124

Chemical Structure : SKLB-0124

CAS No.:

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SKLB-0124 (SKLB0124)

Catalog No.: PC-22381Not For Human Use, Lab Use Only.

SKLB-0124 is a selective, first-in-class degrader for the protein arginine methyltransferase 6 (PRMT6) with EC50 of 15.4 uM for HCC827 cells.

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

    Biological Activity

    SKLB-0124 is a selective, first-in-class degrader for the protein arginine methyltransferase 6 (PRMT6) with EC50 of 15.4 uM for HCC827 cells.
    SKLB-0124 shows significantly reduced inhibitory activity against HCC827 cells and MDA-MB-435 cells with IC50 of 5.9 and 5.1 uM, respectively.
    SKLB-0124 is a selective methyltransferase degrader for PRMT6, but not for PRMT1 and PRMT8.
    SKLB-0124 induced cell cycle arrest and apoptosis in HCC827 cells and MDA-MB-435 cells.

    Physicochemical Properties

    M.Wt 531.75
    Formula C32H45N5O2
    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

    4-(2-((3s)-adamantan-1-yl)acetamido)-N-(4-(5-((methyl(2-(methylamino)ethyl)amino)methyl)pyridin-3-yl)phenyl)butanamide

    References

    1. Hongling Yang, et al. Bioorg Chem. 2024 May 10:148:107439.

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