C188-9

Catalog No.S8605

C188-9 Chemical Structure

Molecular Weight(MW): 471.52

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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Cited by 1 Publication

1 Customer Review

  • (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 M1z1fGZ2dmO2aX;uJIF{e2G7 NVnGR2JVOTBizszN NWTzRW9oOjh4OES0NVk>
SK-N-DZ NG\De5BHfW6ldHnvckBie3OjeR?= M4i3VVExKM7:TR?= NG\MZm0zQDZ6NESxPS=>
Huh7 M3PESWNmdGxidnnhZoltcXS7IHHzd4F6 NGrtWms1QCCq NWTLTol6UUN3ME2xNU4zPyEQvF2= NFTqOGozQDV|M{KyOS=>
PLC/PRF/5 MXjD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NHjTVo01QCCq M1zRXGlEPTB;MUGuPFMh|ryP MkC2Nlg2OzN{MkW=
HepG2 MorLR4VtdCC4aXHibYxqfHliYYPzZZk> M1HSOVQ5KGh? M3i3WmlEPTB;MUCuNVkh|ryP NEnTWVAzQDV|M{KyOS=>
SCC-35 NEHNXIZE\WyuIHfyc5d1cCCjc4PhfS=> NYTpNmx5OC9yLkGvNE4{NzFxMz:xNE8yODBizszN MmfYN|YhcA>? MX7JR|UxRTFyLkigxtEhOC5yIN88US=> M{PVTlI4ODJ5NES1
SCC-61 MX7D[YxtKGe{b4f0bEBie3OjeR?= M331eFAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= NG\EVHo{PiCq MUDJR|UxRTF2LkigxtEzNjlizszN NFzoWpIzPzB{N{S0OS=>
UM-SCC-17B MkTwR4VtdCCpcn;3eIgh[XO|YYm= NFvDWZExNzBwMT:wMlMwOS9|L{GwM|ExOCEQvF2= MX2zOkBp MU\JR|UxRTBwNzFCtUAxNjZizszN M4Xsd|I4ODJ5NES1
HN30 NXLpOnBmS2WubDDndo94fGhiYYPzZZk> M3zkVlAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= MXmzOkBp M3e1dmlEPTB;ND60JOKyKDBwMTFOwG0> M2HPeVI4ODJ5NES1
A549 MonYSpVv[3Srb36gZZN{[Xl? NF;jXIszNjViaB?= NX3U[ZJI\GWlcnXhd4VlKHCVVFHUN{Bt\X[nbIOgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKgd5RienSrbnegZZQh[2:wY3XueJJifGmxboOgZZMhdG:5IHHzJFMhdk1? M3;Bd|I3PDFyMUe3
Kasumi-1 MknrSpVv[3Srb36gZZN{[Xl? NUHLcHE{UUN3ME20MlUh|ryP MYiyNVQ1Pzh|MB?=
THP-1 NF3QS2tHfW6ldHnvckBie3OjeR?= Ml;lTWM2OD12Lkig{txO MlT0NlE1PDd6M{C=
GDM-1 MlXESpVv[3Srb36gZZN{[Xl? MmrpTWM2OD13LkCg{txO NVnQdHRxOjF2NEe4N|A>
NB-1 NUGybJptTnWwY4Tpc44h[XO|YYm= M3q1WmlEPTB;OD6zJO69VQ>? MmPTNlE1PDd6M{C=
HL-60 MlXPSpVv[3Srb36gZZN{[Xl? NEDyRmNKSzVyPUWuN{DPxE1? NFj4d4wzOTR2N{izNC=>
KG-1 NETFXWZHfW6ldHnvckBie3OjeR?= MnXBTWM2OD12LkGg{txO MX[yNVQ1Pzh|MB?=
K562 MnG4RZBweHSxc3nzJIF{e2G7 M2XzTYlv\HWldHnvckBw\iCjcH;weI9{cXNid3n0bEBidiCHQ{WwJI9nKDR|Lk[g{txO MYqyNVQ1Pzh|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]

+ Expand
  • 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]

+ Expand
  • Animal Models: CD2F1 female mice received isogenic C26 tumor cell via s.c injection
  • Formulation: D5W (5g of dextrose in 100 ml of water)
  • 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

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID