C188-9

For research use only.

Catalog No.S8605

16 publications

C188-9 Chemical Structure

CAS No. 432001-19-9

C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

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Selleck's C188-9 has been cited by 16 publications

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  • (E) Hep3B cells were pre-infected with flag-CEP55 for 24 h and were then infected with 10 nM JAK2 inhibitor XL019 or 10 nM STAT3 inhibitor C188-9 for 48 h. Cells’ invasion ability was determined by trans-well assays. Representative microscope images are plotted. Bars, 50 μm;

    Cells, 2018, 7(8). C188-9 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.
Targets
STAT3 [1]
(Cell-free)
4.7 nM(Kd)
In vitro

C188-9 is a 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[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Y79 NHH6PVVHfW6ldHnvckBie3OjeR?= NXHyTmtvOTBizszN MlX6Nlg3QDR2MUm=
SK-N-DZ NEfDeYdHfW6ldHnvckBie3OjeR?= MnTmNVAh|ryP NEPV[4EzQDZ6NESxPS=>
Huh7 NF7Y[pFE\WyuII\pZYJqdGm2eTDhd5NigQ>? NHTmPI01QCCq NHXO[mRKSzVyPUGxMlI4KM7:TR?= MUiyPFU{OzJ{NR?=
PLC/PRF/5 NYewWZpLS2WubDD2bYFjcWyrdImgZZN{[Xl? MnPYOFghcA>? MkXmTWM2OD1zMT64N{DPxE1? NWnOZo4yOjh3M{OyNlU>
HepG2 NFX1Sm1E\WyuII\pZYJqdGm2eTDhd5NigQ>? MYK0PEBp NInIUlVKSzVyPUGwMlE6KM7:TR?= M4qwZlI5PTN|MkK1
SCC-35 NWS0cHhtS2WubDDndo94fGhiYYPzZZk> NHz4WXIxNzBwMT:wMlMwOS9|L{GwM|ExOCEQvF2= NYm3bHIxOzZiaB?= NEDhNG9KSzVyPUGwMlghyrFiMD6wJO69VQ>? NIXhSY8zPzB{N{S0OS=>
SCC-61 NXn5fZA1S2WubDDndo94fGhiYYPzZZk> MlHENE8xNjFxMD6zM|EwOy9zMD:xNFAh|ryP NYi5THdLOzZiaB?= MmrFTWM2OD1zND64JOKyOi57IN88US=> MkfBNlcxOjd2NEW=
UM-SCC-17B NHLUZVBE\WyuIHfyc5d1cCCjc4PhfS=> NULnc4o{OC9yLkGvNE4{NzFxMz:xNE8yODBizszN NVy4dmtrOzZiaB?= MVLJR|UxRTBwNzFCtUAxNjZizszN Mo[wNlcxOjd2NEW=
HN30 NWrYNWhMS2WubDDndo94fGhiYYPzZZk> M4DPcFAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= M2G2UVM3KGh? NXz6Z5E2UUN3ME20MlQhyrFiMD6xJO69VQ>? NHqyTZozPzB{N{S0OS=>
A549 MWXGeY5kfGmxbjDhd5NigQ>? MmnpNk42KGh? M2LV[oRm[3KnYYPl[EBxW1SDVEOgcIV3\Wy|IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{IIP0ZZJ1cW6pIHH0JINwdmOnboTyZZRqd26|IHHzJIxwfyCjczCzJI5O M{nO[VI3PDFyMUe3
Kasumi-1 MWDGeY5kfGmxbjDhd5NigQ>? M376T2lEPTB;ND61JO69VQ>? MUWyNVQ1Pzh|MB?=
THP-1 MkLPSpVv[3Srb36gZZN{[Xl? MlnjTWM2OD12Lkig{txO MmXXNlE1PDd6M{C=
GDM-1 MX7GeY5kfGmxbjDhd5NigQ>? MVXJR|UxRTVwMDFOwG0> NHjSW|czOTR2N{izNC=>
NB-1 M4jIWWZ2dmO2aX;uJIF{e2G7 NWrmXow6UUN3ME24MlMh|ryP NWi5b4NTOjF2NEe4N|A>
HL-60 MlPYSpVv[3Srb36gZZN{[Xl? NYLKUGlQUUN3ME21MlMh|ryP M1LOSFIyPDR5OEOw
KG-1 MoflSpVv[3Srb36gZZN{[Xl? MV3JR|UxRTRwMTFOwG0> NXP6Z5QyOjF2NEe4N|A>
K562 NXrTSZE2SXCxcITvd4l{KGG|c3H5 MYTpcoR2[3Srb36gc4Yh[XCxcITvd4l{KHerdHigZY4hTUN3MDDv[kA1Oy54IN88US=> MV:yNVQ1Pzh|MB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / CEBPδ / Myostatin / p-Akt / Akt ; 

PubMed: 24011072     


C2C12 myotubes were treated with or without C188-9 for 2 h before adding IL-6 (100 ng/ml) for 24 h. A representative western blot for the indicated proteins is shown.

24011072
Immunofluorescence
VE-cadherin / β-catenin; 

PubMed: 26948077     


Confocal microscopy of VE-cadherin (green), total β-catenin (red), and DAPI (blue) in DMSO and C188–9(1µM) pre-treated HUVECs then subsequently exposed to histamine (100 µM). 

non-phosphorylated β-Catenin; 

PubMed: 26948077     


Confocal microscopy of active (non-phosphorylated) β-Catenin (green) and DAPI (blue) in DMSO and C188–9 (1 µM) pre-treated HUVECs then subsequently exposed to histamine (100 µM). 

26948077
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[2].

Protocol

Cell Research:

[2]

- Collapse
  • Cell lines: HNSCC cell line, UM-SCC-17B
  • Concentrations: 0, 0.1, 0.3, 1, 3, 10, 30 μM
  • Incubation Time: 24 h
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: CD2F1 female mice received isogenic C26 tumor cell via s.c injection
  • Dosages: 12.5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (199.35 mM)
Ethanol 6 mg/mL (12.72 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 471.52
Formula

C27H21NO5S

CAS No. 432001-19-9
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC=C(C=C1)S(=O)(=O)NC2=CC(=C(C3=CC=CC=C32)O)C4=C(C=CC5=CC=CC=C54)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID