C188-9

Catalog No.S8605 Synonyms: TTI 101

For research use only.

C188-9 (TTI 101) 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.

C188-9 Chemical Structure

CAS No. 432001-19-9

Selleck's C188-9 has been cited by 32 publications

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Biological Activity

Description C188-9 (TTI 101) 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 MV3GeY5kfGmxbjDhd5NigQ>? MYKxNEDPxE1? Mkf2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OES0NVkoRjJ6Nki0OFE6RC:jPh?=
SK-N-DZ MofMSpVv[3Srb36gZZN{[Xl? MmP0NVAh|ryP M4XRdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6Nki0OFE6Lz5{OE[4OFQyQTxxYU6=
Huh7 MYLD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MX:0PEBp Mki0TWM2OD1zMT6yO{DPxE1? NHfkNok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWzN|IzPSd-Mki1N|MzOjV:L3G+
PLC/PRF/5 NWXRUXN6S2WubDD2bYFjcWyrdImgZZN{[Xl? MnLSOFghcA>? MnfHTWM2OD1zMT64N{DPxE1? NUexW|RGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1N|MzOjVpPkK4OVM{OjJ3PD;hQi=>
HepG2 MmPXR4VtdCC4aXHibYxqfHliYYPzZZk> NYjjS4pmPDhiaB?= NGq5Zo5KSzVyPUGwMlE6KM7:TR?= NIrZ[pA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWzN|IzPSd-Mki1N|MzOjV:L3G+
SCC-35 MlrjR4VtdCCpcn;3eIgh[XO|YYm= M3PFflAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= MkfrN|YhcA>? NYTHNIQ3UUN3ME2xNE45KMLzIECuNEDPxE1? NIjE[WM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CyO|Q1PSd-MkewNlc1PDV:L3G+
SCC-61 NVvyZmtyS2WubDDndo94fGhiYYPzZZk> MUSwM|AvOS9yLkOvNU8{NzFyL{GwNEDPxE1? NXTFeXo1OzZiaB?= MWfJR|UxRTF2LkigxtEzNjlizszN MkjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMke0OFUoRjJ5MEK3OFQ2RC:jPh?=
UM-SCC-17B M12yd2NmdGxiZ4Lve5RpKGG|c3H5 Ml\JNE8xNjFxMD6zM|EwOy9zMD:xNFAh|ryP NVjGeI9wOzZiaB?= MkXNTWM2OD1yLkegxtEhOC54IN88US=> NV7TNVF6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNlc1PDVpPkK3NFI4PDR3PD;hQi=>
HN30 NXjybYZnS2WubDDndo94fGhiYYPzZZk> NXjwbpdnOC9yLkGvNE4{NzFxMz:xNE8yODBizszN MXyzOkBp NUXITVh1UUN3ME20MlQhyrFiMD6xJO69VQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB{N{S0OUc,OjdyMke0OFU9N2F-
A549 M4\SUGZ2dmO2aX;uJIF{e2G7 MnTGNk42KGh? NULsfVh1\GWlcnXhd4VlKHCVVFHUN{Bt\X[nbIOgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKgd5RienSrbnegZZQh[2:wY3XueJJifGmxboOgZZMhdG:5IHHzJFMhdk1? MlLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2MUCxO|coRjJ4NEGwNVc4RC:jPh?=
Kasumi-1 NX3tXo5ZTnWwY4Tpc44h[XO|YYm= M2r4UWlEPTB;ND61JO69VQ>? M{DmbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNES3PFMxLz5{MUS0O|g{ODxxYU6=
THP-1 NHHvUIRHfW6ldHnvckBie3OjeR?= NGrzelRKSzVyPUSuPEDPxE1? M3;zZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNES3PFMxLz5{MUS0O|g{ODxxYU6=
GDM-1 NEjnbXBHfW6ldHnvckBie3OjeR?= MVPJR|UxRTVwMDFOwG0> Mn\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NEe4N|AoRjJzNES3PFMxRC:jPh?=
NB-1 NGCzWWpHfW6ldHnvckBie3OjeR?= Mn3YTWM2OD16LkOg{txO NYnrfIJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
HL-60 M1vZTGZ2dmO2aX;uJIF{e2G7 NVu2emlGUUN3ME21MlMh|ryP M4XRWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNES3PFMxLz5{MUS0O|g{ODxxYU6=
KG-1 M3G3b2Z2dmO2aX;uJIF{e2G7 NF[2UHZKSzVyPUSuNUDPxE1? Mnn1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NEe4N|AoRjJzNES3PFMxRC:jPh?=
K562 MU\BdI9xfG:|aYOgZZN{[Xl? NES2SWdqdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IIfpeIgh[W5iRVO1NEBw\iB2Mz62JO69VQ>? M37VZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNES3PFMxLz5{MUS0O|g{ODxxYU6=
A673 MYHxTHRUKGG|c3H5 MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NXj5V5A{eUiWUzDhd5NigQ>? MYLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NGTNdIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 M17DS5FJXFNiYYPzZZk> MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? M2XUfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD NUHrU5pPeUiWUzDhd5NigQ>? MkLKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ MkHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 M4SwN5FJXFNiYYPzZZk> MV7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? M{HQV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 Mk[zdWhVWyCjc4PhfS=> NEXE[VdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz NGTYOG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 MWnxTHRUKGG|c3H5 M{PldZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) NIjQUpByUFSVIHHzd4F6 MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NFvySYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NHy0SnNyUFSVIHHzd4F6 MkTldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? NILFZWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 M4jxWJFJXFNiYYPzZZk> NW\U[po6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> M{XRb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MkDXdWhVWyCjc4PhfS=> M1\Mb5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MnPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 M1TxSZFJXFNiYYPzZZk> NI\sUW9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NITEcGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MoTQdWhVWyCjc4PhfS=> NVGwWG1keUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz M{TTZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / CEBPδ / Myostatin / p-Akt / Akt 24011072
Immunofluorescence VE-cadherin / β-catenin ; non-phosphorylated β-Catenin 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 (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[1]

  • Animal Models: CD2F1 female mice received isogenic C26 tumor cell via s.c injection
  • Dosages: 12.5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 471.52
Formula

C27H21NO5S

CAS No. 432001-19-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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