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    C188-9
    C188-9

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V3113
    CAS #: 432001-19-9 Purity ≥98%

    Description: C188-9 is a novel, potent and orally bioavailable STAT3 inhibitor that binds to STAT3 with high affinity (KD=4.7±0.4 nM). It is a small-molecule inhibitor that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinase. C188-9 is well tolerated in mice, has good oral bioavailability, and is concentrated in tumors. STAT3 inhibition by C188-9 resulted in attenuated skin fibrosis, myofibroblast accumulation, pro-fibrotic gene expression and collagen deposition in both mouse models of skin fibrosis. C188-9 decreased in vitro dermal fibroblast production of fibrotic genes induced by IL-6 trans-signalling and TGF-β. Finally, TGF-β induced phosphotyrosylation of STAT3 in a SMAD3-dependent manner.

    References:  2015 Apr 24;290(17):11177-87;  2016 May 3;7(18):26307-30.


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    Molecular Weight (MW) 471.52
    Formula C27H21NO5S
    CAS No. 432001-19-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 94 mg/mL (199.4 mM)
    Water: < 1mg/mL
    Ethanol: 6 mg/mL (12.72 mM)
    Solubility (In vivo)
    Synonyms C 188-9; C188-9; C-188-9; C-1889; C 1889; C1889; C-1889; F0808-0084
    SMILES Code O=S(C1=CC=C(OC)C=C1)(NC2=C3C=CC=CC3=C(O)C(C4=C5C=CC=CC5=CC=C4O)=C2)=O


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    In Vitro

    In vitro activity: C188-9 is a potent small-molecule inhibitor of STAT3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases.


    Kinase Assay:


    Cell Assay: UM-SCC-17B cells were incubated with various doses (0/0.1/0.3/1/3/10/30μM) of C188 or C188-9 for 24 hrs.

    In Vivo Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors.
    Animal model CD2F1 female mice received isogenic C26 tumor cell via s.c injection
    Formulation & Dosage D5W (5g of dextrose in 100 ml of water); 12.5 mg/kg; i.p.
    References  2016 May 3;7(18):26307-30;  2015 Apr 24;290(17):11177-87


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    C188-9

    Structure Activity Relationship (SAR) of C188 and similar compounds.  2016 May 3;7(18):26307-30.

     

    C188-9

    Inhibition of STAT3 activities by C188 and C188-9.  2016 May 3;7(18):26307-30.

    C188-9

    C188-9 binds to STAT3 with high affinity.  2016 May 3;7(18):26307-30.


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