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GYS32661

Chemical Structure : GYS32661

CAS No.: 2589092-11-3

GYS32661 (GYS 32661)

Catalog No.: PC-20183Not For Human Use, Lab Use Only.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

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    Biological Activity

    GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
    GYS32661 showed significant inhibition of Rac1 and Rac1b activity at 5 μmol/L in HCT116 colorectal cancer cells.
    GYS32661 (10 uM) significantly blocked Rac1b-mediated NF-κB activity, attenuated TNFα-stimulated NF-κB activity.
    GYS32661 attenuated phosphorylation of both IKBα and RelA/p65, inhibited downstream activation of NF-κB signaling in colorectal cancer. GYS32661sensitized colorectal cancer cells to chemotherapy (Oxaliplatin).
    GYS32661 was shown to have higher activity against both recombinant Rac1 and recombinant Rac1b than EHT1864.
    GYS32661 reduced the growth rates in xenograft models of human CRC in mice.

    Physicochemical Properties

    M.Wt 464.55
    Formula C23H27F3N4OS
    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-((1-(5-((7-(trifluoromethyl)quinolin-4-yl)thio)pentyl)-1H-imidazol-4-yl)methyl)morpholine

    References

    1. Erik T Goka, et al. Mol Cancer Ther. 2019 May;18(5):957-968.

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