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 29 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 NHi4Z|BHfW6ldHnvckBie3OjeR?= NYm3NnJ7OTBizszN MnHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OES0NVkoRjJ6Nki0OFE6RC:jPh?=
SK-N-DZ NITBV2JHfW6ldHnvckBie3OjeR?= M4jZdVExKM7:TR?= MnHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OES0NVkoRjJ6Nki0OFE6RC:jPh?=
Huh7 MkiwR4VtdCC4aXHibYxqfHliYYPzZZk> NUPYR|NbPDhiaB?= M2nXdmlEPTB;MUGuNlch|ryP NVL5Und[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1N|MzOjVpPkK4OVM{OjJ3PD;hQi=>
PLC/PRF/5 NFGwW4VE\WyuII\pZYJqdGm2eTDhd5NigQ>? MWG0PEBp NUDTUWoxUUN3ME2xNU45OyEQvF2= NVvj[nc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1N|MzOjVpPkK4OVM{OjJ3PD;hQi=>
HepG2 NUPJc2M2S2WubDD2bYFjcWyrdImgZZN{[Xl? M13DU|Q5KGh? MXfJR|UxRTFyLkG5JO69VQ>? NIfQbJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWzN|IzPSd-Mki1N|MzOjV:L3G+
SCC-35 NVi4[IJxS2WubDDndo94fGhiYYPzZZk> M2jwOFAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= MlG2N|YhcA>? MUTJR|UxRTFyLkigxtEhOC5yIN88US=> NH2wSnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CyO|Q1PSd-MkewNlc1PDV:L3G+
SCC-61 Mm\nR4VtdCCpcn;3eIgh[XO|YYm= MnnONE8xNjFxMD6zM|EwOy9zMD:xNFAh|ryP NYDscnVIOzZiaB?= MWXJR|UxRTF2LkigxtEzNjlizszN MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB{N{S0OUc,OjdyMke0OFU9N2F-
UM-SCC-17B MlLlR4VtdCCpcn;3eIgh[XO|YYm= MYewM|AvOS9yLkOvNU8{NzFyL{GwNEDPxE1? M3:4b|M3KGh? NF7XTIpKSzVyPUCuO{DDuSByLk[g{txO Mk\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMke0OFUoRjJ5MEK3OFQ2RC:jPh?=
HN30 NEnobVVE\WyuIHfyc5d1cCCjc4PhfS=> M2\4PFAwOC5zL{CuN{8yNzNxMUCvNVAxKM7:TR?= NGDxVYs{PiCq MoXYTWM2OD12LkSgxtEhOC5zIN88US=> MmTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMke0OFUoRjJ5MEK3OFQ2RC:jPh?=
A549 M2LCeGZ2dmO2aX;uJIF{e2G7 NVi2[|N3Oi53IHi= MmXY[IVkemWjc3XkJJBUXEGWMzDs[ZZmdHNiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJic4ThdpRqdmdiYYSgZ49v[2WwdILheIlwdnNiYYOgcI94KGG|IEOgcm0> NW\IXmF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0NVAyPzdpPkK2OFExOTd5PD;hQi=>
Kasumi-1 NH64O5hHfW6ldHnvckBie3OjeR?= MV7JR|UxRTRwNTFOwG0> NW\pcXhNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
THP-1 NVXCOpZxTnWwY4Tpc44h[XO|YYm= NEPUR2xKSzVyPUSuPEDPxE1? NYC2UlZ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
GDM-1 NH;hcZpHfW6ldHnvckBie3OjeR?= MmrYTWM2OD13LkCg{txO NHS0XoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS0O|g{OCd-MkG0OFc5OzB:L3G+
NB-1 M3rKU2Z2dmO2aX;uJIF{e2G7 NYS3OIJVUUN3ME24MlMh|ryP NXPD[npERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
HL-60 MULGeY5kfGmxbjDhd5NigQ>? M4\2ZWlEPTB;NT6zJO69VQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR2N{izNEc,OjF2NEe4N|A9N2F-
KG-1 NFHUZnVHfW6ldHnvckBie3OjeR?= NUfHUlRFUUN3ME20MlEh|ryP NVqzPFhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OFc5OzBpPkKxOFQ4QDNyPD;hQi=>
K562 M1frWmFxd3C2b4Ppd{Bie3OjeR?= M{nRcYlv\HWldHnvckBw\iCjcH;weI9{cXNid3n0bEBidiCHQ{WwJI9nKDR|Lk[g{txO M1LINFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNES3PFMxLz5{MUS0O|g{ODxxYU6=
A673 M3vveJFJXFNiYYPzZZk> MmK2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? NXfLRXZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NYnze3MzeUiWUzDhd5NigQ>? NX\kT|JVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> NHqzdIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 MUHxTHRUKGG|c3H5 M{DxZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD M1K5bZFJXFNiYYPzZZk> NFqyV2hyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 NHrhTXFyUFSVIHHzd4F6 MWDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? M{[3ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 M4TBbZFJXFNiYYPzZZk> M1jIbJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NHLoeXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 NFTicGdyUFSVIHHzd4F6 MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MkL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) MXPxTHRUKGG|c3H5 MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? M{GwT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MYfxTHRUKGG|c3H5 NVvQcFVpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= NH7NPHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MoTFdWhVWyCjc4PhfS=> MVLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MmDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NH[5NmZyUFSVIHHzd4F6 MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M330Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 MoDJdWhVWyCjc4PhfS=> NF\UPYRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NFXJVoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 NGX4VVdyUFSVIHHzd4F6 MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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.

  • (Only for Reference)
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.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 94 mg/mL
(199.35 mM)
Water Insoluble
Ethanol '6 mg/mL

* 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 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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Calculation results:

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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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