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14-3-3σ-ERα stabilizer 181

Chemical Structure : 14-3-3σ-ERα stabilizer 181

CAS No.: 3057296-86-0

14-3-3σ-ERα stabilizer 181 (14-3-3σ/ERα stabilizer 181)

Catalog No.: PC-21138Not For Human Use, Lab Use Only.

14-3-3σ/ERα stabilizer 181 is a selective and highly potent covalent stabilizer of 14-3-3σ/ERα PPI complex with EC50 of 1 uM.

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

    Biological Activity

    14-3-3σ/ERα stabilizer 181 is a selective and highly potent covalent stabilizer of 14-3-3σ/ERα PPI complex with EC50 of 1 uM.
    14-3-3σ/ERα stabilizer 181 shows remarkable selectivity for 14-3-3σ/ERα (appKD of 18 nM), with a similar selectivity profile as Fusicoccin-A (Cat# PC-61233).
    14-3-3σ/ERα stabilizer 181 shows no stabilization of 14-3-3σ/C-RAF, SOS1, ChREBP, p65 and PIN1, up to 150 μM.
    14-3-3σ/ERα stabilizer 181 shows a comparable stabilization profile as Fusicoccin-A.

    Physicochemical Properties

    M.Wt 496.47
    Formula C25H35Cl2N3O3
    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

    2-chloro-1-(9-(4-((4-chlorophenyl)amino)-2,6-dimethyltetrahydro-2H-pyran-4-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)ethan-1-one

    References

    1. Konstantinidou M, et al. J Am Chem Soc. 2023 Sep 7. doi: 10.1021/jacs.3c05161.

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