C188-9

For research use only.

Catalog No.S8605

19 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 190 In stock
USD 127 In stock
USD 390 In stock
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Selleck's C188-9 has been cited by 19 publications

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Choose Selective STAT Inhibitors

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 MoPHSpVv[3Srb36gZZN{[Xl? MmXrNVAh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ6NESxPUc,Ojh4OES0NVk9N2F-
SK-N-DZ MU\GeY5kfGmxbjDhd5NigQ>? MVmxNEDPxE1? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ6NESxPUc,Ojh4OES0NVk9N2F-
Huh7 NEezV|JE\WyuII\pZYJqdGm2eTDhd5NigQ>? Mm\qOFghcA>? MYTJR|UxRTFzLkK3JO69VQ>? NGTMSWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWzN|IzPSd-Mki1N|MzOjV:L3G+
PLC/PRF/5 NGrnSHNE\WyuII\pZYJqdGm2eTDhd5NigQ>? M1;6eVQ5KGh? NGXBRnNKSzVyPUGxMlg{KM7:TR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV|M{KyOUc,Ojh3M{OyNlU9N2F-
HepG2 NYLGcIsyS2WubDD2bYFjcWyrdImgZZN{[Xl? M3PPTFQ5KGh? M3nJemlEPTB;MUCuNVkh|ryP MmjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3M{OyNlUoRjJ6NUOzNlI2RC:jPh?=
SCC-35 MXrD[YxtKGe{b4f0bEBie3OjeR?= M2PleVAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= NIP4WoE{PiCq MWHJR|UxRTFyLkigxtEhOC5yIN88US=> M{jIOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEK3OFQ2Lz5{N{CyO|Q1PTxxYU6=
SCC-61 MV3D[YxtKGe{b4f0bEBie3OjeR?= Mli1NE8xNjFxMD6zM|EwOy9zMD:xNFAh|ryP MVSzOkBp MX7JR|UxRTF2LkigxtEzNjlizszN MlnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMke0OFUoRjJ5MEK3OFQ2RC:jPh?=
UM-SCC-17B NXvKe4tSS2WubDDndo94fGhiYYPzZZk> MlXDNE8xNjFxMD6zM|EwOy9zMD:xNFAh|ryP NEDj[o4{PiCq MXfJR|UxRTBwNzFCtUAxNjZizszN NGTRUYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CyO|Q1PSd-MkewNlc1PDV:L3G+
HN30 NVPaSFl5S2WubDDndo94fGhiYYPzZZk> NXz3ZmpoOC9yLkGvNE4{NzFxMz:xNE8yODBizszN NVPt[3lEOzZiaB?= NYnFcppRUUN3ME20MlQhyrFiMD6xJO69VQ>? M4PqPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEK3OFQ2Lz5{N{CyO|Q1PTxxYU6=
A549 M2rDZ2Z2dmO2aX;uJIF{e2G7 NF7RRmIzNjViaB?= NFPyUHhl\WO{ZXHz[YQheFOWQWSzJIxmfmWuczDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjDzeIFzfGmwZzDheEBkd26lZX70doF1cW:wczDhd{Btd3diYYOgN{BvVQ>? M4XQblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEGwNVc4Lz5{NkSxNFE4PzxxYU6=
Kasumi-1 NFTZfGRHfW6ldHnvckBie3OjeR?= Mo\4TWM2OD12LkWg{txO NYXTV5d4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
THP-1 M2nrSmZ2dmO2aX;uJIF{e2G7 NFeyZVJKSzVyPUSuPEDPxE1? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR2N{izNEc,OjF2NEe4N|A9N2F-
GDM-1 MkjqSpVv[3Srb36gZZN{[Xl? MkTpTWM2OD13LkCg{txO MlruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NEe4N|AoRjJzNES3PFMxRC:jPh?=
NB-1 NFPwU3NHfW6ldHnvckBie3OjeR?= M{DYRWlEPTB;OD6zJO69VQ>? NFO5fG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS0O|g{OCd-MkG0OFc5OzB:L3G+
HL-60 M2DGW2Z2dmO2aX;uJIF{e2G7 MXLJR|UxRTVwMzFOwG0> NWDuOpNzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
KG-1 NUfDTWJCTnWwY4Tpc44h[XO|YYm= NF;3UoVKSzVyPUSuNUDPxE1? NYPW[JRqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
K562 MV3BdI9xfG:|aYOgZZN{[Xl? MUDpcoR2[3Srb36gc4Yh[XCxcITvd4l{KHerdHigZY4hTUN3MDDv[kA1Oy54IN88US=> Ml\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NEe4N|AoRjJzNES3PFMxRC:jPh?=
A673 M{jmVpFJXFNiYYPzZZk> MUjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NEPGR4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MYrxTHRUKGG|c3H5 MoTjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NXTyR2VRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 MkLXdWhVWyCjc4PhfS=> NHm0RYJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= NUXuNlJlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD MkDPdWhVWyCjc4PhfS=> MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NVXI[446RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 MYTxTHRUKGG|c3H5 Ml\wdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| NGn0SVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MVrxTHRUKGG|c3H5 MVXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| Mli4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 MU\xTHRUKGG|c3H5 MmqzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M4PXc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) NIDoUlFyUFSVIHHzd4F6 MmXUdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NUfBVI9CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 MXzxTHRUKGG|c3H5 M1;wbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| MmfUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 NGfxSI1yUFSVIHHzd4F6 M4XuOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz M1u2[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MXvxTHRUKGG|c3H5 NWKzcoZ{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M3;C[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 MofkdWhVWyCjc4PhfS=> MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MoO3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MUnxTHRUKGG|c3H5 MWDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NEjEd2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID