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Stattic

Catalog No. T6308 CAS 19983-44-9

Synonyms: STAT3 Inhibitor V

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

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Stattic, CAS 19983-44-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 77.00
50 mg	In stock	$ 126.00
100 mg	In stock	$ 197.00
200 mg	In stock	$ 293.00
500 mg	In stock	$ 490.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.76%

Purity: 99.64%

Purity: 98.78%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.
Targets&IC50	STAT3:5.1 μM (cell free)
In vitro	METHODS: Human pancreatic cancer cells PANC-1 and BxPc-3 were treated with Stattic (1-10 μM) for 12-48 h. Cell viability was measured using the CCK-8. RESULTS: Stattic decreased the proliferation of PANC-1 and BxPc-3 cells in a concentration- and time-dependent manner, and the IC50s of Stattic on BxPc-3 and PANC-1 cells were 3.135-5.296 μM and 3.835-4.165 μM, respectively, after treatment with Stattic for 24 h. [1] METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Stattic (5-20 μM) for 1 h, followed by stimulation with IL-6 or IFN-γ, and the expression levels of target proteins were detected by Western Blot. RESULTS: Pre-incubation with Stattic resulted in a selective decrease in the phosphorylation of STAT3 Tyr705, while the activation of STAT1 Tyr701 remained unchanged. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Stattic (10 mg/kg) was administered intraperitoneally once daily for four weeks to BALB/c nude mice harboring human pancreatic adenocarcinoma tumor PANC-1. RESULTS: Stattic inhibited PC growth in a nude mouse tumor model by inactivating STAT3. [1] METHODS: To investigate the role in acute liver injury, Stattic (5 mg/kg in DMSO:olive oil = 1:19) was administered as a single intraperitoneal injection to BALB/c mice with LPS/d-GalN induced acute liver injury. RESULTS: Stattic was protective against LPS/d-GalN-induced liver injury, and its protective effect may be related to its anti-inflammatory and anti-apoptotic effects. [3]
Kinase Assay	The screening was performed at approximately 30C. 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 was 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. Peptides were >95% pure. 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 tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Analysis of c-Myc/Max and Jun/Jun dimerization and DNA binding at 37°C was performed as described but in the absence of DTT. Before measurement at room temperature, the mixtures were allowed to equilibrate for at least 30 min. Test compounds were used at the indicated concentrations diluted from 20× stock in DMSO. Binding curves and inhibition curves were fitted with SigmaPlot. All competition curves were repeated three times in independent experiments. For the analysis of time dependence of the inhibition, the components were mixed from stock solutions kept at 0C and then incubated at 37C. Aliquots were taken at the indicated time points [1].
Cell Research	MDA-MB-231, MDA-MB-435S, and MDA-MB-453 cells were seeded. at 5 × 10^4 cells in 6-well plates, grown for 24 hr before adding DMSO or Stattic (final DMSO concentration 0.1%) and then incubated with the inhibitor for 24 hr. All cells were collected and resuspended in buffer (0.1% sodium citrate, 0.1% Triton X-100, 20 μM propidium iodide) and incubated for 3 hr before 10^4 cells per sample were analyzed by flow cytometry with a FACSCalibur equipped with a 488 nm laser [1].

Synonyms	STAT3 Inhibitor V
Molecular Weight	211.19
Formula	C8H5NO4S
CAS No.	19983-44-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 1.1 mg/mL (5 mM)

DMSO: 10.6 mg/mL (50 mM)

References and Literature

1. Guo H, et al. Inhibition of STAT3Y705 phosphorylation by Stattic suppresses proliferation and induces mitochondrial-dependent apoptosis in pancreatic cancer cells. Cell Death Discov. 2022 Mar 14;8(1):116. 2. Schust J, et al. Stattic: a small-molecule inhibitor of STAT3 activation and dimerization. Chem Biol. 2006 Nov;13(11):1235-42. 3. Li S, et al. Stattic alleviates acute hepatic damage induced by LPS/d-galactosamine in mice. Innate Immun. 2021 Feb;27(2):201-209. 4. Zhao C, Zhang B, Jiang J, et al. Up-regulation of ANXA1 suppresses polymorphonuclear neutrophil infiltration and myeloperoxidase activity by activating STAT3 signaling pathway in rat models of myocardial ischemia-reperfusion injury[J]. Cellular signalling. 2019, 62: 109325. 5. Lin I Y, Pan M H, Lai C S, et al. CCM111, the water extract of Antrodia cinnamomea, regulates immune-related activity through STAT3 and NF-κB pathways[J]. Scientific Reports. 2017 Jul 7;7(1):4862. 6. Ning T, Guo J, Zhang K, et al. Nanosecond pulsed electric fields enhanced chondrogenic potential of mesenchymal stem cells via JNK/CREB-STAT3 signaling pathway[J]. Stem cell research & therapy. 2019 Jan 24;10(1):45. 7. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells[J]. Frontiers in immunology. 2020, 11.

Citations

1. Wang X, Li X, Wang J, et al. SMGL-1/NBAS acts as a RAB-8 GEF to regulate unconventional protein secretion. Journal of Cell Biology. 2022, 221(7): e202111125 2. Li K, Fan L, Lin J, et al. Nanosecond pulsed electric fields prime mesenchymal stem cells to peptide ghrelin and enhance chondrogenesis and osteochondral defect repair in vivo. Science China Life Sciences. 2021: 1-13. 3. Zhang T, Wang Y, Li Q, et al. Mesenchymal stromal cells equipped by IFNα empower T cells with potent anti-tumor immunity. Oncogene. 2022: 1-16. 4. Zheng Q W, Ni Q Z, Zhu B, et al. PPDPF promotes lung adenocarcinoma progression via inhibiting apoptosis and NK cell-mediated cytotoxicity through STAT3. Oncogene. 2022: 1-13. 5. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells. Frontiers in immunology. 2021 Jan 29;11:615868. doi: 10.3389/fimmu.2020.615868. eCollection 2020. 6. Ning T, Guo J, Zhang K, et al. Nanosecond pulsed electric fields enhanced chondrogenic potential of mesenchymal stem cells via JNK/CREB-STAT3 signaling pathway. Stem Cell Research & Therapy. 2019 Jan 24;10(1):45 7. Lin I Y, Pan M H, Lai C S, et al. CCM111, the water extract of Antrodia cinnamomea, regulates immune-related activity through STAT3 and NF-κB pathways. Scientific Reports. 2017, 7(1): 1-13 8. Zheng J M, Zhou H X, Yu H Y, et al. By Increasing the Expression and Activation of STAT3, Sustained C5a Stimulation Increases the Proliferation, Migration, and Invasion of RCC Cells and Promotes the Growth of Transgrafted Tumors. Cancer Management and Research. 2021, 13: 7607-7621. 9. Zhao C, Zhang B, Jiang J, et al. Up-regulation of ANXA1 suppresses polymorphonuclear neutrophil infiltration and myeloperoxidase activity by activating STAT3 signaling pathway in rat models of myocardial ischemia-reperfusion injury. Cellular Signalling. 2019, 62: 109325 10. He S, Lu M, Zhang L, et al.RSK4 promotes the macrophage recruitment and M2 polarization in esophageal squamous cell carcinoma.Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease.2023: 166996.

11. Yu L, Xu L, Chen Y, et al.IDO1 Inhibition Promotes Activation of Tumor-intrinsic STAT3 Pathway and Induces Adverse Tumor-protective Effects.The Journal of Immunology.2024 12. Liu H, Sun L, Zhao H, et al.Proteinase 3 depletion attenuates leukemia by promoting myeloid differentiation.Cell Death & Differentiation.2024: 1-14.

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Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Apoptosis Compound Library Anti-Diabetic Compound Library Human Metabolite Library Anti-Cancer Compound Library Anti-Liver Cancer Compound Library Stem Cell Differentiation Compound Library JAK-STAT Compound Library Bioactive Compounds Library Max

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Keywords

Stattic 19983-44-9 Apoptosis JAK/STAT signaling Stem Cells STAT inhibit Alport PC3M-1E8 cancer p-STAT3 prostate S727 syndrome Inhibitor P-ERK1/2 SH2 STAT3 Inhibitor V S phase Y705 inhibitor

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