S3I-201

For research use only.

Catalog No.S1155 Synonyms: NSC 74859

120 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.

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10mM (1mL in DMSO) USD 78 In stock
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Selleck's S3I-201 has been cited by 120 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
BT474R  M3zp[GZ2dmO2aX;uJGF{e2G7 MXS1NEDPxE1? M4PMWlExNTZyIHS= NI[xTGxqdmirYnn0d{BUXEGWMzDhZ5Rqfmm2eR?= NFPJ[2MzPTN{N{W2NS=>
NCI-N87R M1XsT2Z2dmO2aX;uJGF{e2G7 MVG1NEDPxE1? MlrZNVAuPjBiZB?= M13hOYlvcGmkaYTzJHNVSVR|IHHjeIl3cXS7 NYHiZo84OjV|Mke1OlE>
GH3 NFT1SWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVW1NE0yOjVizszN MXy3NkBp M3qyWYF1fGWwdXH0[ZMhfGinIHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX[yOVc4PDVyMx?=
GC  NYXNWmVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml30OVAuOTJ3IN88US=> NUTKcVcyPzJiaB?= NWDLcHN{[XS2ZX71ZZRmeyC2aHWgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUjVeXNIOjV5N{S1NFM>
H460  NHXWUo9CeG:ydH;zbZMhSXO|YYm= MorZNVAxyqCwTR?= MlnRNlTDqGh? M1HzNolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3:teJJm[XSnZDD3bZRpKEKHWkKzOS=> MlLnNlQ1PzJ3M{i=
A459 NVrGU3NlSXCxcITvd4l{KEG|c3H5 NFPkOncyODEEoH7N M4LGeFI1yqCq MWTpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxLYTy[YF1\WRid3n0bEBDTVp{M{W= MVyyOFQ4OjV|OB?=
H460  MlTZRZBweHSxc3nzJGF{e2G7 M1X1OVExOMLibl2= NG\FUpUzPMLiaB?= MX\lcohidmOnczDj[YxtKGSnYYToJINwNXS{ZXH0[YQhf2m2aDDMXVI6PDByMh?= MViyOFQ4OjV|OB?=
MT-2 M3G1dGFxd3C2b4Ppd{BCe3OjeR?= M{\JW|c2NTNyMDFOwG0> MmnONlQwPDhiaB?= M{jVR5N2eHC{ZYPz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGGwZDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{yqB? NImxRoQzPDB7MEm5OS=>
HUT-102 NIH3NJlCeG:ydH;zbZMhSXO|YYm= MUG3OU0{ODBizszN MUSyOE81QCCq NYH4fllZe3WycILld5NmeyClZXzsJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJiYX7kJIlv\HWlZYOgZ4VtdCCjcH;weI9{cXQEoB?= NWDQ[Jl4OjRyOUC5PVU>
U373  M2H4WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DNNlEzPSEQvF2= NHvOVGEzPCCq MojUSG1UVw>? NUe3UW9[\Gm|coXweJMhW1SDVEOgd4lodmGuaX7nJIFv\CCycn;sbYZmemG2aX;u MV2yOFA4ODh{MB?=
T-cell  M{XkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTVyIN88US=> NWHjfmZGOjRyNki3N|E>
H1299 Ml\ISpVv[3Srb36gRZN{[Xl? M1e1XlUxNzFyMDFOwG0> Ml;ROFghcA>? NEXSUHJ{fXCycnXzd4V{KG2rUj25NoEh\XiycnXzd4lwdiCmb4PlMYRmeGWwZHXueIx6 MnXrNlM5OjB{NUS=
H460  MoDHSpVv[3Srb36gRZN{[Xl? MnPMOVAwOTByIN88US=> MUO0PEBp NULLOZNucW6qaXLpeJMhfGinIGP0ZZQ{SyCrbnPy[YF{\WRibXnSMVkz[SCneIDy[ZN{cW:w MYmyN|gzODJ3NB?=
PLC/PRF/5  NVe4TWh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTqVoZROTByIH7N NG\J[Wg1QCCq NH;ldnpFVVOR NXLldld[cW6qaXLpeJMhfGinIFnMMVYhe3SrbYXsZZRqd25icILvcY91\WRiY3XscEBxem:uaX\ldoF1cW:w M3HyPFI{OzZ2M{i5
Huh7 Mn3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\NNVAxKG6P NInEeIo1QCCq MWrEUXNQ NVnkNZdEcW6qaXLpeJMhfGinIFnMMVYhe3SrbYXsZZRqd25icILvcY91\WRiY3XscEBxem:uaX\ldoF1cW:w MV2yN|M3PDN6OR?=
HUVEC  M{DMOGZ2dmO2aX;uJGF{e2G7 NVjDUGFVOC53LUKwJO69VQ>? MX[yOEBp MX3EUXNQ MVjzeZBxemW|c3XzJJRp\SCqeYDvfIliNWmwZIXj[YQh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NVrCTZhVOjF3MkO1OVk>
 U-373 MG M2DhXWN6fG:2b4jpZ4l1gSCDc4PhfS=> MXGzM|ExKM7:TR?= M4L4VlI1KGh? M{TyfJJm\HWlZYOgSm4u|rNvaX7keYNm\CClZXzsJI5mfXKxdH;4bYNqfHl? NF7HPIczODh6OESxOi=>
MDA-MB-231 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmyWZA4OiCq M2HPVGlEPTExvK6xNFAh|ryP NEKwPXYzODB5Mk[1Ni=>
SK-BR-3 MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\qWlczKGh? NH\3Nm9KSzVy78{eNVAxKM7:TR?= NEDCc3YzODB5Mk[1Ni=>
PANC-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fQ[FczKGh? MWnJR|Ux97zgMUCwJO69VQ>? MlnRNlAxPzJ4NUK=
HPAC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFflV2w4OiCq M1TFOWlEPTExvK6xNFAh|ryP NWr4WG9COjByN{K2OVI>
U87 NVe0NFRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP1O|IhcA>? MmPPTWM2OD13NT6xJO69VQ>? NHzlVHEzODB5Mk[1Ni=>
U373  M2jTd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEO2XmQ4OiCq MWXJR|UxRTV{LkWg{txO MlHINlAxPzJ4NUK=

... 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.
6mg/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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID