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SKLB-C05

Chemical Structure : SKLB-C05

CAS No.: 2300981-68-2

SKLB-C05 (TOPK inhibitor SKLB-C05)

Catalog No.: PC-35916Not For Human Use, Lab Use Only.

SKLB-C05 is a novel selective, orally active TOPK inhibitor with IC50 of 0.5 nM, shows excellent cytotoxicity and anti-migration and invasion activity on TOPK high-expressing CRC cells and induces cell apoptosis.

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    Biological Activity

    SKLB-C05 is a novel selective, orally active TOPK inhibitor with IC50 of 0.5 nM, shows excellent cytotoxicity and anti-migration and invasion activity on TOPK high-expressing CRC cells and induces cell apoptosis.
    SKLB-C05 exhibits markedly prioritized inhibitory activity on TOPK-positive CRC cells than TOPK-negative cells (HCT116 cell IC50=96 nM).
    SKLB-C05 inhibits TOPK downstream signaling including ERK1/2, p38, and JNK1/2/3, as well as downregulation of FAK/Src- MMP signaling.
    SKLB-C05 dramatically attenuates CRC tumor xenograft growth and completely suppressed hepatic metastasis of HCT116 cells (20 and 10 mg/kg/day).

    Physicochemical Properties

    M.Wt 394.899
    Formula C23H23ClN2O2
    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

    (S)-1-(4-(1-aminopropan-2-yl)phenyl)-2-hydroxy-4-methylphenanthridin-6(5H)-one hydrochloride

    References

    1. Gao T, et al. Cancer Lett. 2018 Dec 24. pii: S0304-3835(18)30737-7.

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