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CSLP43

Chemical Structure : CSLP43

CAS No.: 2244988-80-3

CSLP43 (RIPK2 inhibitor CSLP43)

Catalog No.: PC-35429Not For Human Use, Lab Use Only.

CSLP43 (RIPK2 inhibitor CSLP43) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 19.9 nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling.

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    Biological Activity

    CSLP43 (RIPK2 inhibitor CSLP43) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 19.9 nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling.
    CSLP43 exhibits inhibition of TNF release from RAW264.7 cells with EC50 of 1.2 nM, inhibits NF-κB reporter activity with IC50 of 1.34 nM.
    CSLP43 antagonizes NOD2 signaling by interfering with the XIAP-RIPK2 interaction, selectively inhibits NOD responses in cells (HEKBlue NOD2 IC50=1.3 nM) and displays potent activity in vivo, does not attenuates the TNF release following an unrelated pro-inflammatory stimulation mediated through TLR4 activation by LPS at 1 uM.

    Physicochemical Properties

    M.Wt 511.641
    Formula C26H33N5O4S
    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-(5-(2-amino-5-(4-(piperazin-1-yl)phenyl)pyridin-3-yl)-2,3-dimethoxyphenyl)propane-1-sulfonamide

    References

    1. Hrdinka M, et al. EMBO J. 2018 Jul 19. pii: e99372.

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