Catalog No.S1155 Synonyms: NSC 74859

S3I-201 Chemical Structure

Molecular Weight(MW): 365.36

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

Size Price Stock Quantity  
In DMSO USD 78 In stock
USD 70 In stock
USD 120 In stock
USD 370 In stock
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Cited by 24 Publications

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Biological Activity

Description S3I-201 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.
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
BT474R  NFjPTG9HfW6ldHnvckBCe3OjeR?= MnXyOVAh|ryP NVjLeYp[OTBvNkCg[C=> MW\pcohq[mm2czDTWGFVOyCjY4Tpeol1gQ>? NHvaOXMzPTN{N{W2NS=>
NCI-N87R MoTJSpVv[3Srb36gRZN{[Xl? M4fHfVUxKM7:TR?= M3zIe|ExNTZyIHS= MWPpcohq[mm2czDTWGFVOyCjY4Tpeol1gQ>? NI\aR|UzPTN{N{W2NS=>
GH3 M1u4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nyT|UxNTF{NTFOwG0> NXjFSJhrPzJiaB?= NEfrNHdifHSnboXheIV{KHSqZTDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkPSNlU4PzR3MEO=
GC  MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;LVFc2OC1zMkWg{txO NYrzTGQ6PzJiaB?= M2OyZoF1fGWwdXH0[ZMhfGinIHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M{LIbFI2Pzd2NUCz
A459 NVXZfllJSXCxcITvd4l{KEG|c3H5 M{nOUVExOMLibl2= M{TVUVI1yqCq MlXzbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClbz30doVifGWmIIfpeIghSkWcMkO1 NYLaU4YzOjR2N{K1N|g>
H460  NF;iXJRCeG:ydH;zbZMhSXO|YYm= NWO1NHk5OTBywrDuUS=> M4fMTFI1yqCq NIjYOVdmdmijbnPld{Bk\WyuIHTlZZRpKGOxLYTy[YF1\WRid3n0bEBNYTJ7NECwNi=> MnKzNlQ1PzJ3M{i=
MT-2 MXzBdI9xfG:|aYOgRZN{[Xl? NWfKS3liPzVvM{CwJO69VQ>? MkfYNlQwPDhiaB?= MoL4d5VxeHKnc4Pld{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZIh[W6mIHnu[JVk\XNiY3XscEBieG:ydH;zbZPDqA>? NH;xXXEzPDB7MEm5OS=>
HUT-102 M3LqVGFxd3C2b4Ppd{BCe3OjeR?= NIK2TZE4PS1|MECg{txO MXiyOE81QCCq NGLkbI9{fXCycnXzd4V{KGOnbHygdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjbnSgbY5lfWOnczDj[YxtKGGyb4D0c5Nqe8Li NXHm[JVmOjRyOUC5PVU>
U373  Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHTNVI2KM7:TR?= MXSyOEBp M2nlVGROW09? NFjsN2xlcXO{dYD0d{BUXEGWMzDzbYdv[WyrbnegZY5lKHC{b3zp[oVz[XSrb36= NYPDcY04OjRyN{C4NlA>
T-cell  Mkj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;KRZVKSzVyPUWwJO69VQ>? MkDBNlQxPjh5M{G=
H1299 M{HJTGZ2dmO2aX;uJGF{e2G7 NILoUWI2OC9zMECg{txO M4nUWlQ5KGh? NIX3VnZ{fXCycnXzd4V{KG2rUj25NoEh\XiycnXzd4lwdiCmb4PlMYRmeGWwZHXueIx6 NGLOT5UzOzh{MEK1OC=>
H460  NFPzeFZHfW6ldHnvckBCe3OjeR?= M33DWlUxNzFyMDFOwG0> M3jWVVQ5KGh? NYPPbIpncW6qaXLpeJMhfGinIGP0ZZQ{SyCrbnPy[YF{\WRibXnSMVkz[SCneIDy[ZN{cW:w MUGyN|gzODJ3NB?=
PLC/PRF/5  NETONVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSxNFAhdk1? MVq0PEBp NXH5RmNZTE2VTx?= NHPYR3RqdmirYnn0d{B1cGViSVytOkB{fGmvdXzheIlwdiCycn;tc5Rm\CClZXzsJJBzd2yrZnXyZZRqd25? NXPaO4JHOjN|NkSzPFk>
Huh7 M4nIW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvxcJI1OTByIH7N MV:0PEBp M13iSGROW09? M3;VUolvcGmkaYTzJJRp\SCLTD22JJN1cW23bHH0bY9vKHC{b33veIVlKGOnbHygdJJwdGmoZYLheIlwdg>? MWWyN|M3PDN6OR?=
HUVEC  MofFSpVv[3Srb36gRZN{[Xl? NUnSb2pSOC53LUKwJO69VQ>? NIG4V2ozPCCq NXe0N|F6TE2VTx?= MmSyd5VxeHKnc4Pld{B1cGViaInwc5hq[S2rbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x NHf4NoIzOTV{M{W1PS=>
 U-373 MG Mke4R5l1d3SxeHnjbZR6KEG|c3H5 MkTTN{8yOCEQvF2= NF6zS3UzPCCq NIj3foNz\WS3Y3XzJGZPNc7|LXnu[JVk\WRiY3XscEBv\XW{b4TvfIlkcXS7 MonENlA5QDh2MU[=
MDA-MB-231 M3TOO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjuSZQ{PzJiaB?= NGTPe4RKSzVy78{eNVAxKM7:TR?= NFfOPFYzODB5Mk[1Ni=>
SK-BR-3 NXnkTIVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjiOVM4OiCq NYjyNVVrUUN3MP-8olExOCEQvF2= M4\YclIxODd{NkWy
PANC-1 NF;lO|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fqVFczKGh? M1vI[WlEPTExvK6xNFAh|ryP NYXWb4RHOjByN{K2OVI>
HPAC NXvOVmg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4q2clczKGh? MnXBTWM2OO,:nkGwNEDPxE1? MY[yNFA4OjZ3Mh?=
U87 NHLZ[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrKd3NPPzJiaB?= M4LOdGlEPTB;NUWuNUDPxE1? NH;0d48zODB5Mk[1Ni=>
U373  Mkm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nh[FczKGh? NHrEdIRKSzVyPUWyMlUh|ryP M3qxd|IxODd{NkWy

... Click to View More Cell Line Experimental Data

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]


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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Human breast cancer MDA-MB-231 cells are injected s.c. into the left flank of athymic nu/nu mice.
  • Formulation: S3I-201 is formulated in DMSO.
  • 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.

* 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


CAS No. 501919-59-1
Storage powder
in solvent
Synonyms NSC 74859

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID