S3I-201

Catalog No.S1155 Synonyms: NSC 74859

For research use only.

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.

S3I-201 Chemical Structure

CAS No. 501919-59-1

Selleck's S3I-201 has been cited by 193 publications

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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 MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LjO|czKGh? NIDzWotKSzVyPUW1MlEh|ryP NH;1cVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC3NlY2Oid-MkCwO|I3PTJ:L3G+
U373  NH7SdVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjVNYtsPzJiaB?= NYrwUld{UUN3ME21Nk42KM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB5Mk[1Nkc,OjByN{K2OVI9N2F-
HPAC NUnld5BnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:3NkBp NEHRWXhKSzVy78{eNVAxKM7:TR?= M4HBSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEeyOlUzLz5{MEC3NlY2OjxxYU6=
PANC-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj3O|IhcA>? MknOTWM2OO,:nkGwNEDPxE1? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB5Mk[1Nkc,OjByN{K2OVI9N2F-
SK-BR-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rvNVczKGh? M2CzS2lEPTExvK6xNFAh|ryP NEPJWYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC3NlY2Oid-MkCwO|I3PTJ:L3G+
 U-373 MG NGPQU3BEgXSxdH;4bYNqfHliQYPzZZk> MnnRN{8yOCEQvF2= M1y3bFI1KGh? NIPlSFNz\WS3Y3XzJGZPNc7|LXnu[JVk\WRiY3XscEBv\XW{b4TvfIlkcXS7 M1Wz[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEi4OFE3Lz5{MEi4PFQyPjxxYU6=
MDA-MB-231 NFfpTodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v4cVczKGh? Mlz4TWM2OO,:nkGwNEDPxE1? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB5Mk[1Nkc,OjByN{K2OVI9N2F-
HUVEC  NYHHeno2TnWwY4Tpc44hSXO|YYm= M{XvdVAvPS1{MDFOwG0> M1nyTlI1KGh? MUXEUXNQ M17HSZN2eHC{ZYPz[ZMhfGinIHj5dI95cWFvaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> NWjrb29XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1NlM2PTlpPkKxOVI{PTV7PD;hQi=>
Huh7 NGnzNWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKxNFAhdk1? MkLLOFghcA>? M{DVXGROW09? MXvpcohq[mm2czD0bIUhUUxvNjDzeIlufWyjdHnvckBxem:vb4Tl[EBk\WyuIIDyc4xq\mW{YYTpc44> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN4NEO4PUc,OjN|NkSzPFk9N2F-
PLC/PRF/5  NWrHUGlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjONGVEOTByIH7N M4KxcVQ5KGh? MnnSSG1UVw>? MWPpcohq[mm2czD0bIUhUUxvNjDzeIlufWyjdHnvckBxem:vb4Tl[EBk\WyuIIDyc4xq\mW{YYTpc44> M{D6S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{[0N|g6Lz5{M{O2OFM5QTxxYU6=
H460  NILlbIJHfW6ldHnvckBCe3OjeR?= NWXVS5VSPTBxMUCwJO69VQ>? MmXZOFghcA>? NW[xdYZicW6qaXLpeJMhfGinIGP0ZZQ{SyCrbnPy[YF{\WRibXnSMVkz[SCneIDy[ZN{cW:w NETVSYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyNFI2PCd-MkO4NlAzPTR:L3G+
H1299 NVe2Snp1TnWwY4Tpc44hSXO|YYm= MorBOVAwOTByIN88US=> M3jNV|Q5KGh? M3;EUpN2eHC{ZYPz[ZMhdWmULUmyZUBmgHC{ZYPzbY9vKGSxc3Wt[IVx\W6mZX70cJk> NGfV[m49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyNFI2PCd-MkO4NlAzPTR:L3G+
T-cell  M3fuNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7EVpdHUUN3ME21NEDPxE1? M2\VZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2ME[4O|MyLz5{NEC2PFc{OTxxYU6=
U373  NUHsVmFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn3V|ZrOTJ3IN88US=> NEX2cHAzPCCq MkTsSG1UVw>? NWPhVY5b\Gm|coXweJMhW1SDVEOgd4lodmGuaX7nJIFv\CCycn;sbYZmemG2aX;u MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5MEiyNEc,OjRyN{C4NlA9N2F-
HUT-102 MWHBdI9xfG:|aYOgRZN{[Xl? M3;4fFc2NTNyMDFOwG0> MoPGNlQwPDhiaB?= MoO4d5VxeHKnc4Pld{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[W6mIHnu[JVk\XNiY3XscEBieG:ydH;zbZPDqA>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB7MEm5OUc,OjRyOUC5PVU9N2F-
MT-2 M{HpWWFxd3C2b4Ppd{BCe3OjeR?= M2jKRVc2NTNyMDFOwG0> M{K1O|I1NzR6IHi= MY\zeZBxemW|c3XzJINmdGxicILvcIln\XKjdHnvckBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBidmRiaX7keYNmeyClZXzsJIFxd3C2b4Ppd:Kh MkX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOUC5PVUoRjJ2MEmwPVk2RC:jPh?=
H460  MlHNRZBweHSxc3nzJGF{e2G7 NEXKOFMyODEEoH7N M2\BVVI1yqCq NGfa[2NmdmijbnPld{Bk\WyuIHTlZZRpKGOxLYTy[YF1\WRid3n0bEBNYTJ7NECwNi=> NHmweWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NlU{QCd-MkS0O|I2Ozh:L3G+
A459 NVnXZ404SXCxcITvd4l{KEG|c3H5 MmntNVAxyqCwTR?= MUmyOOKhcA>? MY\pcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxLYTy[YF1\WRid3n0bEBDTVp{M{W= NFLaepc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES3NlU{QCd-MkS0O|I2Ozh:L3G+
H460  NXjnO3BqSXCxcITvd4l{KEG|c3H5 NETF[|AyODEEoH7N NHHIO44zPMLiaB?= NUPsXmZEcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDjc{11emWjdHXkJJdqfGhiQlXaNlM2 M4flNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEeyOVM5Lz5{NES3NlU{QDxxYU6=
GC  NWLKdY5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFThT3I2OC1zMkWg{txO NEf5S4s4OiCq NH\uTnZifHSnboXheIV{KHSqZTDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd5NEWwN{c,OjV5N{S1NFM9N2F-
GH3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGyR4lmPTBvMUK1JO69VQ>? M4rrS|czKGh? MlvLZZR1\W63YYTld{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M1\xZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{e0OVA{Lz5{NUe3OFUxOzxxYU6=
BT474R  Ml;ISpVv[3Srb36gRZN{[Xl? NGT4[HQ2OCEQvF2= NYHoO2g6OTBvNkCg[C=> M{nvNolvcGmkaYTzJHNVSVR|IHHjeIl3cXS7 Mlf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|Mke1OlEoRjJ3M{K3OVYyRC:jPh?=
NCI-N87R NGDBTHJHfW6ldHnvckBCe3OjeR?= Moj0OVAh|ryP MkXTNVAuPjBiZB?= NHLKeHJqdmirYnn0d{BUXEGWMzDhZ5Rqfmm2eR?= M{nmVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{K3OVYyLz5{NUOyO|U3OTxxYU6=
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NIH3T3 NUOwU|U1TnWwY4Tpc44h[XO|YYm= MUSxNFAhfU1? NWXDWVF1OjRiaILz MkXTVoVlfWO2aX;uJI9nKHCWeYKtO|A2KFO2YYSzJIxmfmWuIHnuJJYuW3KlIHX4dJJme3OrbnegcY92e2ViTlnIN3Q{KGOnbHzzJIF1KDFyMDD1UUBi\nSncjCyOEBpenN? NEPldWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
NIH3T3 NYjZeYdjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3mxRlExOCC3TR?= M{fV[|Qh\GG7cx?= NHq4e5VIem:5dHigbY5pcWKrdHnvckBw\iCvb4Xz[UBPUUh|VEOgZ4VtdHNiZYjwdoV{e2mwZzD2MXNz[yCjdDCxNFAhfU1iYX\0[ZIhPCCmYYnzJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigQ>? NHLxd2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
MDA-MB-435 NIi0RoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUOxNFAhfU1? NYfmfWU1PCCmYYnz MVTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHX4dJJme3Orbnegek1UemNiYYSgNVAxKHWPIHHmeIVzKDRiZHH5d{BjgSC2conwZY4h[my3ZTDlfINtfXOrb36gZZN{[Xl? NIPBXJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
MDA-MB-231 MnnrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4HEUFExOCC3TR?= M2XIO|Qh\GG7cx?= MXnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHX4dJJme3Orbnegek1UemNiYYSgNVAxKHWPIHHmeIVzKDRiZHH5d{BjgSC2conwZY4h[my3ZTDlfINtfXOrb36gZZN{[Xl? M3e0U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NE[zNFkxLz5zN{S2N|A6ODxxYU6=
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NIH3T3 NYD0[lVLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvRfoFSOTByIIXN M1XhPWdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUDOWMzDj[YxteyCneIDy[ZN{cW6pII[tVoF{KGG2IEGwNEB2VSCob4Kg[ZZmenliMzDkZZl{KGK7IIPv[pQu[WejcjDjc4xwdnlvZn;ycYF1cW:wIHHzd4F6 MmfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NkOwPVAoRjF5NE[zNFkxRC:jPh?=
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MDA-MB-231 NV35bFk{SXCxcITvd4l{KGG|c3H5 MnvLNVAxKHWP M4PsRlI1KGi{cx?= NFPkenVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJHN1[XR|IGPINkBld22jaX6geJJidnOoZXP0[YQhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDheEAyODBidV2gZYZ1\XJiMkSgbJJ{ NEK1R489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
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NIH3T3 NX3CZVE4TnWwY4Tpc44h[XO|YYm= NWrJT|FKOTByIIXN NVXWS|JsPDhiaILz NFruNVZT\WS3Y4Tpc44hd2ZiY4njcIlvKERzIHflcoUh\XiycnXzd4lwdiCrbjD2MXNz[yC2cnHud4Zm[3SnZDDtc5V{\SCQSVizWFMh[2WubIOgZZQhOTByIIXNJIFnfGW{IES4JIhzew>? NFXRU289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
NIH3T3 NHHRemJHfW6ldHnvckBie3OjeR?= NHLjWIIyODBidV2= MVu0PEBpenN? M{XBOHJm\HWldHnvckBw\iCEY3ytfGwh\2WwZTDlfJBz\XO|aX;uJIlvKHZvU4LjJJRz[W6|ZnXjeIVlKG2xdYPlJG5KUDOWMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILz NE\mNXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
NIH3T3 NInEV41HfW6ldHnvckBie3OjeR?= NGHOOmsyODBidV2= NYq1Rnl3PDhiaILz NF\3fIpT\WS3Y4Tpc44hd2Zic4Xyeol3cW5iZ3Xu[UBmgHC{ZYPzbY9vKGmwII[tV5JkKHS{YX7z[oVkfGWmIH3veZNmKE6LSEPUN{Bk\WyuczDheEAyODBidV2gZYZ1\XJiNEigbJJ{ Mkn0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NkOwPVAoRjF5NE[zNFkxRC:jPh?=
MDA-MB-231 MULGeY5kfGmxbjDhd5NigQ>? NGn0bowyODBidV2= M1TmPVQ5KGi{cx?= M4rFT3Jm\HWldHnvckBw\iCEY3ytfGwh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhOTByIIXNJIFnfGW{IES4JIhzew>? M1jpUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NE[zNFkxLz5zN{S2N|A6ODxxYU6=
MDA-MB-231 NG[xWJNHfW6ldHnvckBie3OjeR?= MnXlNVAxKHWP MXS0PEBpenN? MWTS[YR2[3Srb36gc4Yhe3W{dnn2bY4h\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhOTByIIXNJIFnfGW{IES4JIhzew>? M4LDV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NE[zNFkxLz5zN{S2N|A6ODxxYU6=
MDA-MB-231 NFTNRo9CdnSrdIXtc5Ih[XO|YYm= MWO1JI1oN2up NEDvVFMzKHenZXvz NYjWcpFvSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDlfJBz\XO|aX7nJIFkfGm4ZTDTeIF1OyC6ZX7v[5Ji\nSnZDDpckBud3W|ZTDheEA2KG2pL3vnMEBqfiCob4Kg[ZZmenliMzDkZZl{KG[xcjCyJJdm\Wu| NIT5N249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2N|A6OCd-MUe0OlMxQTB:L3G+
NIH3T3 M2\wUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX7meIhYOTByIIXN MW\Hdo94fGhiaX7obYJqfGmxbjDv[kBud3W|ZTDOTWg{XDNiY3XscJMh\XiycnXzd4lv\yC4LWPyZ{BifCBzMECgeW0h\m:{IHX2[ZJ6KDNiZHH5d{BjgSC|b3\0MYFo[XJiY3;sc456NW[xcn3heIlwdiCjc4PhfS=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR4M{C5NEc,OTd2NkOwPVA9N2F-
A673 NFTSbpRyUFSVIHHzd4F6 NXjUeYhyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= Ml7qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MVjxTHRUKGG|c3H5 NFPlfYdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M4PIO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NF;zblRyUFSVIHHzd4F6 M3nKSZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NX;jXoM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Assay
Methods Test Index PMID
Western blot STAT3 / p-STAT3 / Cyclin D1 / Bcl-2 / Nanog / OCT4 / ALDH1 / CD44 ; PD-L1 26556875 28605599
Immunofluorescence p-STAT3 ; Oct4 / Twist 26556875 27521216
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 365.36
Formula

C16H15NO7S

CAS No. 501919-59-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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