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SCP1 inhibitor GR-28

Chemical Structure : SCP1 inhibitor GR-28

CAS No.:

SCP1 inhibitor GR-28 (GR-28)

Catalog No.: PC-22168Not For Human Use, Lab Use Only.

SCP1 inhibitor GR-28 is a covalent small molecule inhibitor of small C-terminal domain phosphatase 1 (SCP1) with kinact/KI 1383 min-1 M-1, causes degrades REST protein in REST-dependent glioblastoma cells.

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    Biological Activity

    SCP1 inhibitor GR-28 is a covalent small molecule inhibitor of small C-terminal domain phosphatase 1 (SCP1) with kinact/KI 1383 min-1 M-1, causes degrades REST protein in REST-dependent glioblastoma cells.
    GR-28 inhibits SCP1 capacity to dephosphorylate REST leading to accumulation of phospho-REST and its subsequent proteasomal degradation in vitro.
    SCP1 inhibitor GR-28 covalently targets SCP1 Cys 181, and SCP1 C181A mutant shows resistance to GR-28 inhibition.
    SCP1 inhibitor GR-28 (4 uM) reduces the transcriptional activity of REST and GR-28 (10 uM) is cytotoxic against high-REST GBM cells.
    SCP1 inhibitor GR-28 exhibits profound synergy with ACSL inhibitor Triacsin C in high-REST GBM cells.

    Physicochemical Properties

    M.Wt 476.55
    Formula C26H24N2O5S
    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-(3-(2'-methoxy-[1,1'-biphenyl]-4-carboxamido)propyl)cinnamamide 1,1-dioxide

    References

    1. Svetlana B Panina, et al. BMC Biol. 2024 Apr 12;22(1):83.

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