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StatticSTAT3 inhibitor,small-molecule and potent

Stattic

Catalog No. A2224
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
25mg $80.00 In stock
100mg $200.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Stattic

Related Biological Data

Stattic

Related Biological Data

Stattic

Related Biological Data

Stattic

Related Biological Data

Stattic

Biological Activity

Description Stattic is a small-molecule inhibitor of STAT3 with IC50 values of 2.562 ± 0.409 μM, 3.481 ± 0.953 μM, 2.282 ± 0.423 μM and 2.648 ± 0.542 μM in UM-SCC-17B, OSC-19, Cal33 and UM-SCC-22B cell lines, respectively.
Targets STAT3 STAT3 STAT3 STAT3    
IC50 2.562 ± 0.409 μM (UM-SCC-17B cell line) 3.481 ± 0.953 μM (OSC-19 cell line) 2.282 ± 0.423 μM (Cal33 cell line) 2.648 ± 0.542 μM (UM-SCC-22B cell line)    

Protocol

Kinase experiment [1]:

High-throughput screening and fluorescence polarization assays

Screening was performed at approximately 30°C. The specificity of screening hits was validated in analogous assays for binding of the test compounds to the SH2 domains of STAT1, STAT5, and Lck. The final concentration of buffer components used for all FP assays is 10 mM HEPES (pH 7.5), 1 mM EDTA, 0.1% Nonidet P-40, 50 mM NaCl and 10% DMSO. The absence of dithiothreitol is essential for inhibitory activity. The sequences of the peptides were: STAT3, 5-carboxyfluorescein-GY(PO3H2)LPQTV-NH2; STAT1, 5-carboxyfluorescein-GY(PO3H2)DKPHVL; STAT5, 5-carboxyfluorescein-GY(PO3H2)LVLDKW; and Lck, 5-carboxyfluorescein-GY(PO3H2)EEIP. For specificity analysis at 30°C, proteins were used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37 °C, proteins were used at 370 nM (STAT3) or 100 nM (Lck). Proteins were incubated with test compounds in Eppendorf tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Before measurement at room temperature, the mixtures were allowed to equilibrate for at least 30 mins. Test compounds were used at the indicated concentrations diluted from a 20× stock in DMSO. Binding curves and inhibition curves were fitted with SigmaPlot. All competition curves were repeated three times in independent experiment.

Cell experiment [2]:

Cell lines

Head and neck squamous cell carcinoma (HNSCC) cell lines UM-SCC-17B, OSC-19, Cal33, and UM-SCC-22B

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0 ~ 100 M; 24 hrs

Applications

Stattic significantly inhibited STAT3 activation and expression, leading to decreased cell survival and proliferation as well as increased radiosensitivity. The Stattic treatment also reduced STAT3-mediated HIF-1 expression.

Animal experiment [2]:

Animal models

UM-SCC-17B cells xenografted mouse model

Dosage form

50 mg/kg; p.o.; 5 days a week for 4 weeks

Applications

In a murine orthotopic xenograft, oral administration of Stattic effectively reduced the growth of HNSCC tumors, and analysis of tumor lysates validated decreased STAT3 phosphorylation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Jochen Schust, Bianca Sperl, Angela Hollis, Thomas U. Mayer, and Thorsten Berg. Stattic: A Small-Molecule Inhibitor of STAT3 Activation and Dimerization. Chemistry & Biology. 2006(13):1235-1242.

[2]. Makoto Adachi, Caixia Cui, Cristina T. Dodge, Mihir K. Bhayani, Stephen Y. Lai. Targeting STAT3 inhibits growth and enhances radiosensitivity in head and neck squamous cell carcinoma. Oral Oncology. 2012 July(48):1220-1226.

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Chemical Properties

Cas No. 19983-44-9 SDF Download SDF
Chemical Name 6-nitro-1-benzothiophene 1,1-dioxide
Canonical SMILES C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]
Formula C8H5NO4S M.Wt 211.19
Solubility >10.6mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Stattic is a small molecule inhibitor of STAT3 with IC50 values of 2.562 ± 0.409 μM, 3.481 ± 0.953 μM, 2.282 ± 0.423 μM and 2.648 ± 0.542 μM, respectively, in UM-SCC-17B, OSC-19, Cal33 and UM-SCC-22B cell lines [1].

Stattic is reported to selectively inhibit dimerization, activation and nuclear translocation of STAT3. It can also induce the apoptosis of STAT3-dependent breast cancer cell lines [2].

The inhibition of STAT3 by Stattic results in decreased STAT3-mediated HIF-1 expression and subsequent radiosensitization of HNSCC cells. Inhibiting the STAT3 signaling pathway may represent an effective strategy in the treatment of HNSCC. The evidence of Stattic activity in vivo has also been found. Stattic pre-treatment sensitizes orthotopic xenograft HNSCC tumors to radiation, wich results in significantly reduced tumor growth, although this effect was not as dramatic as anticipated by the in vitro studies [1].

References:
[1] Makoto Adachi, Caixia Cui, Cristina T. Dodge, Mihir K. Bhayani, Stephen Y. Lai. Targeting STAT3 inhibits growth and enhances radiosensitivity in head and neck squamous cell carcinoma. Oral Oncology. 2012 July(48):1220-1226.

[2] Jochen Schust, Bianca Sperl, Angela Hollis, Thomas U. Mayer, and Thorsten Berg. Stattic: A Small-Molecule Inhibitor of STAT3 Activation and Dimerization. Chemistry & Biology. 2006(13):1235-1242.