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PAIR1

Chemical Structure : PAIR1

CAS No.: 2771006-58-5

PAIR1 (IRE1α inhibitor PAIR1)

Catalog No.: PC-49055Not For Human Use, Lab Use Only.

PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity.

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    Biological Activity

    PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity.
    Unlike KIRAs, PAIR1 partially displaces helix-αC from an active conformation, and only reduce IRE1α's dimerization affinity.
    PAIR1 spares XBP1 splicing but blocks Regulated IRE1α Dependent Degradation (RIDD) outputs in cells.
    PAIR1 largely preserved XBP1 mRNA splicing and expression of the frame-shifted Xbp1s transcription factor protein in cellular systems.
    PAIR1 inhibits IRE1α-dependent mRNA decay and apoptosis in INS-1 cells that conditionally overexpress IRE1α.
    PAIR1 affect B-lymphocytes to differentiate into immunoglobulin-producing plasma cells.

    Physicochemical Properties

    M.Wt 558.580
    Formula C26H25F3N6O3S
    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-(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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