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S3I-201

(CAS No:501919-59-1)
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.
CAS No:501919-59-1
Molecular Weight(MW):365.36
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 501919-59-1
Molecular formula(MF) C16H15NO7S
Molecular Weight(MW): 365.36
Alias NSC 74859;
Solubility
In vitro DMSO 73 mg/mL (199.8 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+corn oil 6mg/mL
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  Function Assay 50 μM 10-60 d inhibits STAT3 activity 25327561
NCI-N87R Function Assay 50 μM 10-60 d inhibits STAT3 activity 25327561
GH3 Growth Inhibition Assay 50-125 μM 72 h attenuates the cell growth in a dose-dependent manner 25774503
GC  Growth Inhibition Assay 50-125 μM 72 h attenuates the cell growth in a dose-dependent manner 25774503
H460  Apoptosis Assay 100 nM 24 h induces cell apoptosis co-treated with BEZ235 24472538
A459 Apoptosis Assay 100 nM 24 h induces cell apoptosis co-treated with BEZ235 24472538
H460  Apoptosis Assay 100 nM 24 h enhances cell death co-treated with LY294002 24472538
MT-2 Apoptosis Assay 75-300 μM 24/48 h suppresses cell proliferation in a dose-dependent manner and induces cell apoptosis  24090995
HUT-102 Apoptosis Assay 75-300 μM 24/48 h suppresses cell proliferation in a dose-dependent manner and induces cell apoptosis  24090995
U373  Growth Inhibition Assay 125 μM 24 h DMSO disrupts STAT3 signaling and proliferation 24070820
T-cell  Growth Inhibition Assay IC50=50 μM 24068731
H1299 Function Assay 50/100 μM 48 h suppresses miR-92a expression dose-dependently 23820254
H460  Function Assay 50/100 μM 48 h inhibits the Stat3C increased miR-92a expression 23820254
PLC/PRF/5  Growth Inhibition Assay 100 nM 48 h DMSO inhibits the IL-6 stimulation promoted cell proliferation 23364389
Huh7 Growth Inhibition Assay 100 nM 48 h DMSO inhibits the IL-6 stimulation promoted cell proliferation 23364389
HUVEC  Function Assay 0.5-20 μM 24 h DMSO suppresses the hypoxia-induced accumulation of HIF-1α 21523559
 U-373 MG Cytotoxicity Assay 3/10 μM 24 h reduces FN-γ-induced cell neurotoxicity 20888416
MDA-MB-231 Growth Inhibition Assay 72 h IC50＞100 μM 20072652
SK-BR-3 Growth Inhibition Assay 72 h IC50＞100 μM 20072652
PANC-1 Growth Inhibition Assay 72 h IC50＞100 μM 20072652
HPAC Growth Inhibition Assay 72 h IC50＞100 μM 20072652
U87 Growth Inhibition Assay 72 h IC50=55.1 μM 20072652
U373  Growth Inhibition Assay 72 h IC50=52.5 μM 20072652

... 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]
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