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SMIP-30

Chemical Structure : SMIP-30

CAS No.: 2919466-30-9

SMIP-30 (SMIP30, PPM1A inhibitor)

Catalog No.: PC-72527Not For Human Use, Lab Use Only.

SMIP-30 is a potent and selective inhibitor of PPM1A with IC50 of 1 uM, selectively inhibits the phosphatase activity of PPM1A.

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    Biological Activity

    SMIP-30 is a potent and selective inhibitor of PPM1A with IC50 of 1 uM, selectively inhibits the phosphatase activity of PPM1A.
    SMIP-30 shows poor inhibitory activity against closest homolog PPM1B (IC50>30 uM).
    SMIP-30 is an uncompetitive inhibitor for PPM1A (Ki=0.84 uM), does not exhibit any cytotoxic effects up to 30 uM in THP-1 macrophages.
    SMIP-30 dose-dependently reduces the Mtb burden in infected macrophages, and is well tolerated in vivo and combined with rifampicin reduces Mtb burden in the lungs of infected mice.
    SMIP-30 induces LC3B-II expression, activates autophagy in Mtb-infected macrophages in a PPM1A-dependent manner.
    SMIP-30 induces a dose-dependent increase in phosphorylation of S403-p62 in WT macrophages.

    Physicochemical Properties

    M.Wt 352.203
    Formula C16H15BrFNO2
    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-fluoro-5-(2-hydroxyethyl)-8-methoxyphenanthridin-5-ium bromide

    References

    1. Stefania Berton, et al. Cell Chem Biol. 2022 Mar 18;S2451-9456(22)00094-0.

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