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You are here:Home-Chemical Inhibitors & Agonists-JAK/STAT Signaling-JAK-VVD-118313
VVD-118313

Chemical Structure : VVD-118313

CAS No.: 2875046-27-6

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VVD-118313 (VVD118313)

Catalog No.: PC-49343Not For Human Use, Lab Use Only.

VVD-118313 (VVD118313) is a potent, selective and allosteric inhibitor of the non-catalytic pseudokinase domain of JAK1 (C817), blocks JAK1-dependent trans-phosphorylation and cytokine signaling.

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

    Biological Activity

    VVD-118313 (VVD118313) is a potent, selective and allosteric inhibitor of the non-catalytic pseudokinase domain of JAK1 (C817), blocks JAK1-dependent trans-phosphorylation and cytokine signaling.
    VVD-118313 does not impair JAK2-dependent cytokine signaling and are inactive in cells expressing a C817A JAK1 mutant.
    VVD-118313 inhibits IFNα-stimulated STAT1 phosphorylatio with IC50 of 32 nM.
    VVD-118313 selectively inhibits JAK1 by engagement of C817.
    VVD-118313 potently inhibits JAK1-dependent IFNα-pSTAT1, IL-6-pSTAT3, and IL-2-pSTAT5 pathways in human PBMCs, while sparing JAK2- and TYK2/JAK2-dependent signaling.
    VVD-118313 potently inhibits STAT3 phosphorylation in splenocytes from Tyk2−/− mice.
     

    Physicochemical Properties

    M.Wt 429.356
    Formula C19H22Cl2N2O3S
    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

    1-((S)-3-(3,4-dichlorophenyl)piperidin-1-yl)-3-((R)-1-(methylsulfonyl)pyrrolidin-3-yl)prop-2-yn-1-one

    References

    1. Kavanagh ME, et, al. Nat Chem Biol. 2022 Dec;18(12):1388-1398.

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