S3I-201

For research use only.

Catalog No.S1155 Synonyms: NSC 74859

177 publications

S3I-201 Chemical Structure

CAS No. 501919-59-1

S3I-201 (NSC 74859) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.

Selleck's S3I-201 has been cited by 177 publications

Purity & Quality Control

Choose Selective STAT Inhibitors

Biological Activity

Description S3I-201 (NSC 74859) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.
Features A chemical probe inhibitor of Stat3 activity.
Targets
STAT3 [1]
(Cell-free assay)
86 μM
In vitro

S3I-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3 by inhibiting Stat3·Stat3 complex formation and Stat3 DNA-binding and transcriptional activitie. Moreover, S3I-201 also inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin. [1] S3I-201 inhibits breast carcinoma MDA-MB-435, MDA-MB-453 and MDA-MB-231 cell lines with IC50 of 100 μM. In addition, the cells with impaired TGF-β signaling are four times as sensitive to the STAT3 inhibitor S3I-201. [2] A recent study shows that S3I-201 potentiates the antiproliferative effect of cetuximab in HepG2 and Huh-7 cells via the STAT3 signalling pathway. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87 NXT6SJljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDGO|IhcA>? MlfiTWM2OD13NT6xJO69VQ>? M1LrW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEeyOlUzLz5{MEC3NlY2OjxxYU6=
U373  NVvOZZNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTLSHE4OiCq MWjJR|UxRTV{LkWg{txO NF64Ulk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC3NlY2Oid-MkCwO|I3PTJ:L3G+
HPAC NVXzZ3dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle2O|IhcA>? NGDyT4pKSzVy78{eNVAxKM7:TR?= NYnZeHpnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwO|I3PTJpPkKwNFczPjV{PD;hQi=>
PANC-1 NYjPc2FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnXVXc4OiCq M136fGlEPTExvK6xNFAh|ryP NHPafm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC3NlY2Oid-MkCwO|I3PTJ:L3G+
SK-BR-3 M{\BTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO1UYtCPzJiaB?= NE[4UY5KSzVy78{eNVAxKM7:TR?= NGDWSXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC3NlY2Oid-MkCwO|I3PTJ:L3G+
 U-373 MG NGDEN2NEgXSxdH;4bYNqfHliQYPzZZk> Mn7zN{8yOCEQvF2= NV62WHVNOjRiaB?= NF;kWHJz\WS3Y3XzJGZPNc7|LXnu[JVk\WRiY3XscEBv\XW{b4TvfIlkcXS7 NWTDWlBVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFg1OTZpPkKwPFg5PDF4PD;hQi=>
MDA-MB-231 M1ixVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPZR4U4OiCq MV3JR|Ux97zgMUCwJO69VQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB5Mk[1Nkc,OjByN{K2OVI9N2F-
HUVEC  NXi5eWNnTnWwY4Tpc44hSXO|YYm= Mo\WNE42NTJyIN88US=> MXOyOEBp MYDEUXNQ NVrZUpdbe3WycILld5NmeyC2aHWgbJlxd3irYT3pcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCKSV[tNe6y MmnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3MkO1OVkoRjJzNUKzOVU6RC:jPh?=
Huh7 NX3k[mo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;1PXkyODBibl2= MnLuOFghcA>? M3jDSGROW09? M4PhNolvcGmkaYTzJJRp\SCLTD22JJN1cW23bHH0bY9vKHC{b33veIVlKGOnbHygdJJwdGmoZYLheIlwdg>? M{jUO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{[0N|g6Lz5{M{O2OFM5QTxxYU6=
PLC/PRF/5  MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ixV|ExOCCwTR?= NVjrVYl6PDhiaB?= Ml7RSG1UVw>? NGrQdFFqdmirYnn0d{B1cGViSVytOkB{fGmvdXzheIlwdiCycn;tc5Rm\CClZXzsJJBzd2yrZnXyZZRqd25? NXjvNFVHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOlQ{QDlpPkKzN|Y1Ozh7PD;hQi=>
H460  NGXVUlBHfW6ldHnvckBCe3OjeR?= NUT6SJRGPTBxMUCwJO69VQ>? NHnOOIc1QCCq MXrpcohq[mm2czD0bIUhW3SjdEPDJIlv[3KnYYPl[EBucVJvOULhJIV5eHKnc4Ppc44> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh{MEK1OEc,OjN6MkCyOVQ9N2F-
H1299 NYe3UW5OTnWwY4Tpc44hSXO|YYm= NWT4OWR4PTBxMUCwJO69VQ>? NWG5R|d7PDhiaB?= NIPFdVB{fXCycnXzd4V{KG2rUj25NoEh\XiycnXzd4lwdiCmb4PlMYRmeGWwZHXueIx6 M{DHSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEKwNlU1Lz5{M{iyNFI2PDxxYU6=
T-cell  MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonLTWM2OD13MDFOwG0> MmLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNki3N|EoRjJ2ME[4O|MyRC:jPh?=
U373  MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTldYRUOTJ3IN88US=> M2nVVlI1KGh? MYjEUXNQ NFS2RVVlcXO{dYD0d{BUXEGWMzDzbYdv[WyrbnegZY5lKHC{b3zp[oVz[XSrb36= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5MEiyNEc,OjRyN{C4NlA9N2F-
HUT-102 NVix[W5DSXCxcITvd4l{KEG|c3H5 NIXrNlM4PS1|MECg{txO M1zWWFI1NzR6IHi= NHTrU2Z{fXCycnXzd4V{KGOnbHygdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjbnSgbY5lfWOnczDj[YxtKGGyb4D0c5Nqe8Li NGHaVWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5NFk6PSd-MkSwPVA6QTV:L3G+
MT-2 NVzET|hKSXCxcITvd4l{KEG|c3H5 NVXHXXhSPzVvM{CwJO69VQ>? MnO0NlQwPDhiaB?= MkD6d5VxeHKnc4Pld{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[W6mIHnu[JVk\XNiY3XscEBieG:ydH;zbZPDqA>? NI\QWHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5NFk6PSd-MkSwPVA6QTV:L3G+
H460  MW\BdI9xfG:|aYOgRZN{[Xl? NVOxeWdEOTBywrDuUS=> NUfPVnhrOjUEoHi= NGCxXIRmdmijbnPld{Bk\WyuIHTlZZRpKGOxLYTy[YF1\WRid3n0bEBNYTJ7NECwNi=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5MkWzPEc,OjR2N{K1N|g9N2F-
A459 MXPBdI9xfG:|aYOgRZN{[Xl? NGf2XlMyODEEoH7N MYeyOOKhcA>? NEDnXGdqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHPvMZRz\WG2ZXSge4l1cCCERWqyN|U> NXvlOGMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O|I2OzhpPkK0OFczPTN6PD;hQi=>
H460  MoW4RZBweHSxc3nzJGF{e2G7 NHPod2oyODEEoH7N NIW5NlYzPMLiaB?= NY\McG5{cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDjc{11emWjdHXkJJdqfGhiQlXaNlM2 NWXReGczRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O|I2OzhpPkK0OFczPTN6PD;hQi=>
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GH3 NHuxR2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVO1NE0yOjVizszN M4nSfVczKGh? MUnheJRmdnWjdHXzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NFX4c3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe3OFUxOyd-MkW3O|Q2ODN:L3G+
BT474R  MlPhSpVv[3Srb36gRZN{[Xl? NEX0TXk2OCEQvF2= M1[2TVExNTZyIHS= MkTmbY5pcWKrdIOgV3RCXDNiYXP0bZZqfHl? NVG0d405RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNlc2PjFpPkK1N|I4PTZzPD;hQi=>
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MDA-MB-231 MoHHRZBweHSxc3nzJIF{e2G7 M3zwNFExOCC3TR?= NGrXOZkzPCCqcoO= MWnJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIGP0ZZQ{SyC2cnHud4Zm[3SnZDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG2IEGwNEB2VSCjZoTldkAzPCCqcoO= NIj6SWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
NIH3T3 NF3u[5RHfW6ldHnvckBie3OjeR?= NEDWeIoyODBidV2= MoPiOFghcHK| MnP1VoVlfWO2aX;uJI9nKGO7Y3zpckBFOSCpZX7lJIV5eHKnc4Ppc44hcW5idj3TdoMhfHKjboPm[YN1\WRibX;1d4UhVkmKM2SzJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpM> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR4M{C5NEc,OTd2NkOwPVA9N2F-
NIH3T3 MXXGeY5kfGmxbjDhd5NigQ>? M3vrSFExOCC3TR?= MYG0PEBpenN? NYDhbYFCWmWmdXP0bY9vKG:oIFLjcE15VCCpZX7lJIV5eHKnc4Ppc44hcW5idj3TdoMhfHKjboPm[YN1\WRibX;1d4UhVkmKM2SzJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpM> NEPkcFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
NIH3T3 MnjVSpVv[3Srb36gZZN{[Xl? MnzCNVAxKHWP NFXCfYE1QCCqcoO= M3zTXXJm\HWldHnvckBw\iC|dYL2bZZqdiCpZX7lJIV5eHKnc4Ppc44hcW5idj3TdoMhfHKjboPm[YN1\WRibX;1d4UhVkmKM2SzJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpM> NHf0T3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
MDA-MB-231 NIPnNHBHfW6ldHnvckBie3OjeR?= NXvJZWs4OTByIIXN M4j4N|Q5KGi{cx?= MVPS[YR2[3Srb36gc4YhSmOuLYjMJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpM> MnvkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NkOwPVAoRjF5NE[zNFkxRC:jPh?=
MDA-MB-231 MkfzSpVv[3Srb36gZZN{[Xl? M3XMNlExOCC3TR?= NH;udo41QCCqcoO= M3;ienJm\HWldHnvckBw\iC|dYL2bZZqdiCpZX7lJIV5eHKnc4Ppc44hcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BifCBzMECgeW0h[W[2ZYKgOFghcHK| MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR4M{C5NEc,OTd2NkOwPVA9N2F-
MDA-MB-231 NI[wTJFCdnSrdIXtc5Ih[XO|YYm= NGXRbXo2KG2pL3vn NU\afZJPOiC5ZXXrdy=> NIXBVVVCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHX4dJJme3OrbnegZYN1cX[nIGP0ZZQ{KHinbn;ndoFnfGWmIHnuJI1wfXOnIHH0JFUhdWdxa3esJIl3KG[xcjDleoVzgSB|IHThfZMh\m:{IEKge4Vmc3N? MoWyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NkOwPVAoRjF5NE[zNFkxRC:jPh?=
NIH3T3 MoHBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1zIcFExOCC3TR?= M4PmXGdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUDOWMzDj[YxteyCneIDy[ZN{cW6pII[tV5JkKGG2IEGwNEB2VSCob4Kg[ZZmenliMzDkZZl{KGK7IIPv[pQu[WejcjDjc4xwdnlvZn;ycYF1cW:wIHHzd4F6 NYH2cnU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0OlMxQTBpPkG3OFY{ODlyPD;hQi=>
A673 MlrEdWhVWyCjc4PhfS=> NWmwfGZpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= Mkj2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MVjxTHRUKGG|c3H5 MojMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MlrHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 Mn7tdWhVWyCjc4PhfS=> NX\T[lFXeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 MX;xTHRUKGG|c3H5 M132U5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MmDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
STAT3 / p-STAT3 / Cyclin D1 / Bcl-2 / Nanog / OCT4 / ALDH1 / CD44; 

PubMed: 26556875     


Western blotting shows S3I-201 treatment decrease Cyclin D1, Bcl2 and self-renewal marker Nanog, OCT4, ALDH1, and CD44 in a dose dependent manner. Data shown are representative of three individual experiments.

PD-L1; 

PubMed: 28605599     


The expression level of PD-L1 was measured by Western blotting in a head and neck squamous cell carcinoma cell line (Cal 27 and FaDu), with and without S3I-201. β-Actin was used as the internal protein loading control. PD-L1, programmed death 1 ligand; STAT, signal transducers and activators of transcription; p-STAT3, phosphorylated STAT3.

26556875 28605599
Immunofluorescence
p-STAT3; 

PubMed: 26556875     


Immunoflurosece shows S3I-201 reduce nuclear expression of p-STAT3Tyr705 by confocal microscope. 

Oct4 / Twist ; 

PubMed: 27521216     


Suppression of Oct4 and Twist expression was shown in TW01 CD44/CD24 co-overexpressed cells and CSCs after S3I-201 treatment. Scale bars indicate 20 μm.

26556875 27521216
Growth inhibition assay
Cell viability; 

PubMed: 26813676     


The STAT3 inhibitor (S3I-201) decreases cellular proliferation in HTLV-I/ATL-lines. Cells were treated with 0, 12.5, 25, or 50 μM S3I-201 or dimethyl sulfoxide (DMSO) for 72 hours. The average growth curve is representative of the percentage of proliferation between S3I-201 and DMSO-treated cells. Each cell line was treated at least twice for standard deviation. 1185 (-IL2) cells were washed in phosphate-buffered saline and resuspended in media without IL2, followed by treatment with S3I-201 for 72 hours.

26813676
In vivo S3I-201 (5 mg/kg, i.v. every 2 or every 3 days) shows the antitumor efficacy in mouse models with human breast tumor xenografts that harbor constitutively active Stat3. [1] S3I-201 treatment reduces Varicella-zoster virus (VZV) replication on the basis of the bioluminescence signal and the number of positive skin xenografts compared with DMSO-treated mice by inhibiting STAT3 phosphorylation. [4]

Protocol

Kinase Assay:[1]
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In vitro Stat3 DNA-binding assay and EMSA analysis :

Briefly, 100 mL of biotinyl-e-Ac-EPQpYEEIEL-OH (in 50 mM Tris/150 mM NaCl, pH 7.5) is added to each well of streptavidin-coated 96-well microtiter plates and incubated with shaking at 4 °C overnight. Then plates are rinsed with PBS/Tween 20 and then two times with 200 mL of BSA-T-PBS (0.2% BSA/0.1% Tween 20/PBS). Then 50 mL of Lck-SH2-GST fusion protein (6.4 ng/ml in BSA-T-PBS) is added to each well of the 96-well plate in the presence and absence of 50 mL of S3I-201 (for 30 and 100 mM final concentrations), and the plate is shaken at room temperature for 4 hours. After solutions are removed, each well is rinsed four times with BSA-T-PBS (200 mL), and 100 mL of polyclonal rabbit anti-GST antibody (100 ng/mL in BSA-T-PBS) is added to each well and incubated at 4 °C overnight. After washing with BSA-T-PBS, 100 mL of 200 ng/mL BSA-T-PBS horseradish peroxidase-conjugated mouse anti-rabbit antibody is added to each well and incubated for 45 minutes at room temperature. After four washing steps with BSA-T-PBS and three washing steps with PBS-T, 100 mL of peroxidase substrate is added to each well and incubated for 5-15 minutes. The peroxidase reaction is stopped by adding 100 mL of 1 M sulfuric acid solution, and absorbance is read at 450 nm with an ELISA plate rea
Cell Research:[2]
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  • Cell lines: MDA-MB-435, MDA-MB-453 and MDA-MB-231 cells lines
  • Concentrations: ~ 250 μM
  • Incubation Time: 72 hours
  • Method: The MTT assay is based on the conversion of the yellow tetrazolium salt MTT to purple formazan crystals by metabolically active cells. The MTT assay provides a quantitative determination of viable cells. Cells are seeded in 96-well microplates in complete culture medium in the absence or presence of increasing serial dosages of S3I-201 as indicated. At 72 hours after culture, the number of viable cells is measured by adding 100 μL/well of 2 mg/mL MTT solution. After 2 hours, the medium is removed, and the formazan crystals are dissolved by adding 100 μL dimethylsulfoxide per well. The absorbance is read at 590 nm with an enzyme-linked immunosorbent assay reader. Each treatment point is performed in 10 wells or sextuplicate.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Human breast cancer MDA-MB-231 cells are injected s.c. into the left flank of athymic nu/nu mice.
  • Dosages: ≤5 mg/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.8 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
3mg/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 365.36
Formula

C16H15NO7S

CAS No. 501919-59-1
Storage powder
in solvent
Synonyms NSC 74859
Smiles CC1=CC=C(C=C1)S(=O)(=O)OCC(=O)NC2=CC(=C(C=C2)C(=O)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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STAT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID