S3I-201

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 61 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.
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  NFyyPJZHfW6ldHnvckBCe3OjeR?= M37jRVUxKM7:TR?= NF:wdIMyOC14MDDk NH;lUmlqdmirYnn0d{BUXEGWMzDhZ5Rqfmm2eR?= NE[3TJAzPTN{N{W2NS=>
NCI-N87R Mkn1SpVv[3Srb36gRZN{[Xl? M4TEclUxKM7:TR?= MlTvNVAuPjBiZB?= MnnDbY5pcWKrdIOgV3RCXDNiYXP0bZZqfHl? M4KzW|I2OzJ5NU[x
GH3 M1GwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK1NE0yOjVizszN NIfTRVk4OiCq MYrheJRmdnWjdHXzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Ml30NlU4PzR3MEO=
GC  NH7Rdo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3oOVAuOTJ3IN88US=> MXO3NkBp Ml7UZZR1\W63YYTld{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NXrhS4J7OjV5N{S1NFM>
H460  NWfYPGxzSXCxcITvd4l{KEG|c3H5 M3rVdlExOMLibl2= MnTyNlTDqGh? MYrpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxLYTy[YF1\WRid3n0bEBDTVp{M{W= MkL6NlQ1PzJ3M{i=
A459 NHLKVoZCeG:ydH;zbZMhSXO|YYm= MX[xNFDDqG6P M2\1O|I1yqCq M2izOYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3:teJJm[XSnZDD3bZRpKEKHWkKzOS=> NEO4SGMzPDR5MkWzPC=>
H460  MkTSRZBweHSxc3nzJGF{e2G7 Mo\tNVAxyqCwTR?= M3\1VFI1yqCq M1XjVoVvcGGwY3XzJINmdGxiZHXheIgh[29vdILlZZRm\CC5aYToJGx[Ojl2MECy M4\RcVI1PDd{NUO4
MT-2 NIj1N41CeG:ydH;zbZMhSXO|YYm= NXTpSZZJPzVvM{CwJO69VQ>? MWqyOE81QCCq NXfIT2I2e3WycILld5NmeyClZXzsJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJiYX7kJIlv\HWlZYOgZ4VtdCCjcH;weI9{cXQEoB?= NXvldXczOjRyOUC5PVU>
HUT-102 NYrpN|dmSXCxcITvd4l{KEG|c3H5 NXfXS2pjPzVvM{CwJO69VQ>? NVHabG1pOjRxNEigbC=> M4H4O5N2eHC{ZYPz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGGwZDDpcoR2[2W|IHPlcIwh[XCxcITvd4l{yqB? MYWyOFA6ODl7NR?=
U373  NHKwO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3S0O|EzPSEQvF2= MmXONlQhcA>? NG\KPFlFVVOR M{nReIRqe3K3cITzJHNVSVR|IIPp[45idGmwZzDhcoQheHKxbHnm[ZJifGmxbh?= MUKyOFA4ODh{MB?=
T-cell  M4LYN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LHWmlEPTB;NUCg{txO MV[yOFA3QDd|MR?=
H1299 NWm4S|dYTnWwY4Tpc44hSXO|YYm= NVXuRYlwPTBxMUCwJO69VQ>? NYK0bXB{PDhiaB?= Ml[wd5VxeHKnc4Pld{BucVJvOULhJIV5eHKnc4Ppc44h\G:|ZT3k[ZBmdmSnboTsfS=> M3uzbVI{QDJyMkW0
H460  MUnGeY5kfGmxbjDBd5NigQ>? NWTUVWc4PTBxMUCwJO69VQ>? MYC0PEBp NHPUTFlqdmirYnn0d{B1cGViU4TheFNEKGmwY4LlZZNm\CCvaWKtPVJiKGW6cILld5Nqd25? M1jURVI{QDJyMkW0
PLC/PRF/5  Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHKboxZOTByIH7N NEXVcIo1QCCq NHHL[I1FVVOR M3X2TYlvcGmkaYTzJJRp\SCLTD22JJN1cW23bHH0bY9vKHC{b33veIVlKGOnbHygdJJwdGmoZYLheIlwdg>? Mn6zNlM{PjR|OEm=
Huh7 NEHxdJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXrZpgyODBibl2= MlftOFghcA>? MnzISG1UVw>? NILncYdqdmirYnn0d{B1cGViSVytOkB{fGmvdXzheIlwdiCycn;tc5Rm\CClZXzsJJBzd2yrZnXyZZRqd25? M13hOVI{OzZ2M{i5
HUVEC  NVTiWJhPTnWwY4Tpc44hSXO|YYm= NYrz[lBMOC53LUKwJO69VQ>? MmXJNlQhcA>? M1LUfWROW09? MkTMd5VxeHKnc4Pld{B1cGViaInwc5hq[S2rbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x M3noSlIyPTJ|NUW5
 U-373 MG NUXJU4JiS3m2b4TvfIlkcXS7IFHzd4F6 MnLQN{8yOCEQvF2= NX3XT3pXOjRiaB?= MoDYdoVlfWOnczDGUk3Puy2rbnT1Z4VlKGOnbHygcoV2em:2b4jpZ4l1gQ>? MUCyNFg5QDRzNh?=
MDA-MB-231 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3ZNm05PzJiaB?= NWe1SnpMUUN3MP-8olExOCEQvF2= MnzLNlAxPzJ4NUK=
SK-BR-3 NGfhWYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLEO|IhcA>? MofHTWM2OO,:nkGwNEDPxE1? Ml3PNlAxPzJ4NUK=
PANC-1 MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFToVIU4OiCq Ml35TWM2OO,:nkGwNEDPxE1? NWXVNoZkOjByN{K2OVI>
HPAC NX\wNmtET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXewbIx1PzJiaB?= MkHSTWM2OO,:nkGwNEDPxE1? NV25[VdEOjByN{K2OVI>
U87 NX3Db3pIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn75O|IhcA>? M13NdmlEPTB;NUWuNUDPxE1? MoD4NlAxPzJ4NUK=
U373  NGDWfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjacIM4OiCq NYnOe3hLUUN3ME21Nk42KM7:TR?= NXr6VWdQOjByN{K2OVI>

... 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]
+ Expand

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.
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID