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YK-2-69

Chemical Structure : YK-2-69

CAS No.: 2619846-89-6

YK-2-69 (DYRK2 inhibitor YK-2-69)

Catalog No.: PC-38751Not For Human Use, Lab Use Only.

YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM).

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    Biological Activity

    YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM).
    YK-2-69 specifically interacts with Lys-231 and Lys-234 of DYRK2.
    YK-2-69 remarkably reduces PCa burden in vitro and in vivo.
    YK-2-69 exhibits more potent anti-PCa efficacy than the first-line drug enzalutamide in vivo.
    YK-2-69 displays favorable safety properties with a maximal tolerable dose of more than 10,000 mg/kg and pharmacokinetic profiles with 56% bioavailability.

    Physicochemical Properties

    M.Wt 506.604
    Formula C25H27FN8OS
    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

    (6-((4-(2-(dimethylamino)benzo[d]thiazol-6-yl)-5-fluoropyrimidin-2-yl)amino)pyridin-3-yl)(4-ethylpiperazin-1-yl)methanone

    References

    1. Yuan K, et al. Nat Commun. 2022 May 25;13(1):2903.

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