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HTH-02-006

Chemical Structure : HTH-02-006

CAS No.:

HTH-02-006

Catalog No.: PC-73284Not For Human Use, Lab Use Only.

HTH-02-006 is a potent, selective reversible inhibitor of NUAK1/2 with binding IC50 of 8/126 nM, respectively.

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    Biological Activity

    HTH-02-006 is a potent, selective reversible inhibitor of NUAK1/2 with binding IC50 of 8/126 nM, respectively.
    HTH-02-006 reduces MYPT1(S445) phosphorylation in HuCCT-1 cells, suggesting NUAK1/2 inhibition.
    HTH-02-006 ameliorates YAP(S127A)-induced hepatomegaly, and reduces MYPT1(S445) phosphorylation.
    HTH-02-006 delays the outgrowth of YAP-induced HuCCT-1 xenograft tumors in nude mice.
    HTH-02-006 downregulated E2F, EMT, and MYC hallmark gene sets after NUAK2 inhibition in PC cells.
    HTH-02-006 slowed tumor growth and proliferation rates in a syngeneic allograft model and in radical prostatectomy patient derived explants.
    HTH-02-006 treatment led to inactivation of YAP and the downregulation of NUAK2 and MYC protein levels.

    Physicochemical Properties

    M.Wt 588.450
    Formula C25H29IN6O3
    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

    N-(3-((5-iodo-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin4-yl)oxy)phenyl)propionamide

    References

    1. Weiwei Fu, et al. Mol Carcinog. 2022 Mar;61(3):334-345.

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