Stattic

Alias: 6-Nitro-1-benzothiophene 1,1-dioxide
Cat No.:V1380 Purity: ≥98%
Stattic (6-Nitro-1-benzothiophene 1,1-dioxide) isa small molecule inhibitor of STAT3 that potently inhibits STAT3 activation and nuclear translocation with potential antineoplastic activity.
Stattic Chemical Structure CAS No.: 19983-44-9
Product category: STAT
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Stattic (6-Nitro-1-benzothiophene 1,1-dioxide) is a small molecule inhibitor of STAT3 that potently inhibits STAT3 activation and nuclear translocation with potential antineoplastic activity. It inhibits STAT3 with an IC50 of 5.1 μM in cell-free assays, and exhibits high selectivity for STAT3 over STAT1. Stattic is the first nonpeptidic 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. 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In the ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines lacking P-ERK1/ 2, stattic (20 μM; 24 hours) preferentially inhibits P-STAT3 and inhibits STAT3 phosphorylation (Y705), as evidenced by the suppression of [1]. In PC3M-1E8 cells, stattic (2.5, 5, 10 μM; 4 hours) dramatically decreased the nuclear levels of survivin and pSTAT3 at 10 μM. A dose-dependent way is observed in the inhibition of IL-6-induced STAT3 activation by Stattic (2.5-10 μM; 24 hours) [2]. PC3M-1E8 cells, which are prostate cancer cells, exhibit growth inhibition and apoptosis in response to stattic (2.5, 5, 10 μM; 48 hours). At 2.5 μM and 5 μM, stattic does not significantly cause apoptosis [2]. Stattic (2.5, 5, 10 μM; 48 hours) exhibits a notable buildup of S-phase [2]. Stattic leads in very low levels of STAT3 phosphorylation and neither major morphological alterations nor apoptosis in A2780 cells or HUVEC cells [2].
ln Vivo
In Alport syndrome (AS) mice, stattic (10 mg/kg; intraperitoneal injection; three times a week for ten weeks) improves renal dysfunction [3].
Animal Protocol
Animal/Disease Models: Age-matched wild-type (WT) C57BL/6 mice[3]
Doses: 10 mg/kg
Route of Administration: IP; three timesper week for 10 week
Experimental Results: Increased levels of proteinuria, BUN and serum creatinine. Dramatically suppressed the gene expression levels of renal injury markers (Lcn2, Kim-1), pro-inflammatory cytokines (Il-6, KC), pro-fibrotic genes (Tgf-β, Col1a1, α-Sma) and Mmp9.
References
[1]. Lin L, et al. STAT3 as a potential therapeutic target in ALDH+ and CD44+/CD24+ stem cell-like pancreatic cancer cells. Int J Oncol. 2016 Oct 12.
[2]. John S McMurray, et al. A new small-molecule Stat3 inhibitor. Chem Biol. 2006 Nov;13(11):1123-4.
[3]. Tsubasa Yokota, et al. STAT3 inhibition attenuates the progressive phenotypes of Alport syndrome mouse model. Nephrol Dial Transplant. 2018 Feb 1;33(2):214-223.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C8H5NO4S
Molecular Weight
211.19
CAS #
19983-44-9
SMILES
S1(C([H])=C([H])C2C([H])=C([H])C(=C([H])C1=2)[N+](=O)[O-])(=O)=O
Synonyms
6-Nitro-1-benzothiophene 1,1-dioxide
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 42 mg/mL (198.9 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
2%DMSO+30%PEG 300+H2O:8 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.7351 mL 23.6754 mL 47.3507 mL
5 mM 0.9470 mL 4.7351 mL 9.4701 mL
10 mM 0.4735 mL 2.3675 mL 4.7351 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • Stattic

  • Stattic

  • Stattic

  • Stattic

    STAT3 silencing inhibits the tumor growth of human ABC-like DLBCL Ly3 cells xenografts.Cancer Res.2011 May 1;71(9):3182-8.
  • Stattic

    STAT3 silencing induces tumor apoptosis and affects infiltration of tumor microenvironment cells in Ly3 xenografts.Cancer Res.2011 May 1;71(9):3182-8.
  • Stattic

    Small-molecule STAT3 inhibitors affect the growth of Ly3 cells in vitro and in vivo.Cancer Res.2011 May 1;71(9):3182-8.
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