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PAIR2

Chemical Structure : PAIR2

CAS No.: 2771006-54-1

PAIR2 (IRE1α inhibitor PAIR2)

Catalog No.: PC-49054Not For Human Use, Lab Use Only.

PAIR2 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=8.8 nM) but only partially inhibits its RNase activity.

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    Biological Activity

    PAIR2 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=8.8 nM) but only partially inhibits its RNase activity.
    Unlike KIRAs, PAIR2 partially displaces helix-αC from an active conformation, and only reduce IRE1α's dimerization affinity.
    PAIR2 demonstrated a similar ability to inhibit IRE1α's kinase activity as KIRA8 in vitro and in cells.
    PAIR2 affect B-lymphocytes to differentiate into immunoglobulin-producing plasma cells.
    PAIR2 is capable of completely occupying IRE1α's ATP-binding site in cells and can block the ability of a potent KIRA to inhibit XBP1 splicing.

    Physicochemical Properties

    M.Wt 590.598
    Formula C27H26F4N6O3S
    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)-2,2,2-trifluoro-N-(2-fluoro-3-methyl-4-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)ethane-1-sulfonamide

    References

    1. Feldman HC, et al. Nat Chem Biol. 2021 Nov;17(11):1148-1156.

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