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 MlTwSpVv[3Srb36gZZN{[Xl? MWCxNEDPxE1? MkjZNlg3QDR2MUm=
SK-N-DZ M{LWSGZ2dmO2aX;uJIF{e2G7 MV[xNEDPxE1? NYfOSYRnOjh4OES0NVk>
Huh7 NUWzRWxkS2WubDD2bYFjcWyrdImgZZN{[Xl? MVW0PEBp MkXvTWM2OD1zMT6yO{DPxE1? NYnXV5JiOjh3M{OyNlU>
PLC/PRF/5 NVrPS|F{S2WubDD2bYFjcWyrdImgZZN{[Xl? NHjEdFg1QCCq MkLyTWM2OD1zMT64N{DPxE1? M1rRN|I5PTN|MkK1
HepG2 NXjqc3c2S2WubDD2bYFjcWyrdImgZZN{[Xl? MkH0OFghcA>? M2L1OGlEPTB;MUCuNVkh|ryP MX:yPFU{OzJ{NR?=
SCC-35 NFTBTlZE\WyuIHfyc5d1cCCjc4PhfS=> NF7nOHIxNzBwMT:wMlMwOS9|L{GwM|ExOCEQvF2= NG\oW2U{PiCq NXjDZ3lDUUN3ME2xNE45KMLzIECuNEDPxE1? M3LGUVI4ODJ5NES1
SCC-61 NYiyUGFzS2WubDDndo94fGhiYYPzZZk> NGK5XYwxNzBwMT:wMlMwOS9|L{GwM|ExOCEQvF2= MoTEN|YhcA>? NFXqcphKSzVyPUG0MlghyrF{Lkmg{txO M{D5[|I4ODJ5NES1
UM-SCC-17B M{HHTmNmdGxiZ4Lve5RpKGG|c3H5 NGHCfGgxNzBwMT:wMlMwOS9|L{GwM|ExOCEQvF2= MkfQN|YhcA>? NXXnS5M5UUN3ME2wMlchyrFiMD62JO69VQ>? MVeyO|AzPzR2NR?=
HN30 NGrMboRE\WyuIHfyc5d1cCCjc4PhfS=> MlG3NE8xNjFxMD6zM|EwOy9zMD:xNFAh|ryP MXSzOkBp MWHJR|UxRTRwNDFCtUAxNjFizszN NGizSoIzPzB{N{S0OS=>
A549 MXXGeY5kfGmxbjDhd5NigQ>? Mme2Nk42KGh? MXnk[YNz\WG|ZXSgdHNVSVR|IHzleoVteyCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meiC|dHHyeIlv\yCjdDDjc45k\W62cnH0bY9veyCjczDsc5ch[XNiMzDuUS=> M4rQb|I3PDFyMUe3
Kasumi-1 MlPrSpVv[3Srb36gZZN{[Xl? MljOTWM2OD12LkWg{txO NYjqO5pGOjF2NEe4N|A>
THP-1 NUSySVNLTnWwY4Tpc44h[XO|YYm= NW[2Sm5KUUN3ME20Mlgh|ryP NFrCNFQzOTR2N{izNC=>
GDM-1 NGLsRW5HfW6ldHnvckBie3OjeR?= MX3JR|UxRTVwMDFOwG0> NXHzcnhNOjF2NEe4N|A>
NB-1 M4S4SWZ2dmO2aX;uJIF{e2G7 M33m[mlEPTB;OD6zJO69VQ>? NHT1VlQzOTR2N{izNC=>
HL-60 Mom1SpVv[3Srb36gZZN{[Xl? NE\LUGxKSzVyPUWuN{DPxE1? NX7OdHVHOjF2NEe4N|A>
KG-1 NV7O[ItRTnWwY4Tpc44h[XO|YYm= NVjzU4FiUUN3ME20MlEh|ryP MXeyNVQ1Pzh|MB?=
K562 MoHZRZBweHSxc3nzJIF{e2G7 NVzXUVlXcW6mdXP0bY9vKG:oIHHwc5B1d3OrczD3bZRpKGGwIFXDOVAhd2ZiNEOuOkDPxE1? NWLFT2JZOjF2NEe4N|A>

... Click to View More Cell Line Experimental Data

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.

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STAT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID