Stattic

製品コードS7024 バッチS702404

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₈H₅NO₄S
	分子量	211.19	CAS No.	19983-44-9
Solubility (25°C)*	体外	DMSO	42 mg/mL (198.87 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.
in vitro	Stattic inhibits binding of a phosphotyrosine-containing peptide derived from the gp130 receptor to the STAT3 SH2 domain in a strongly temperature-dependent manner. Stattic only has a very weak effect on binding of a tyrosinephosphorylated peptide to the SH2-domain of the tyrosine kinase Lck. And it doesn’t inhibit dimerization of two other dimeric transcription factors (c-Myc/Max and Jun/Jun). It also inhibits fluorescein-labeled phosphopeptides to the SH2 domains of STAT1 and STAT5b. Stattic selectively inhibits DNA binding of STAT3 homodimers at a concentration of 10 μM. Shown to inhibit cellular phosphorylation of STAT3 at Tyr705 with little effect towards STAT1 phosphorylation at Tyr701 (in HepG2 cells) or the phosphorylation of JAK1, JAK2, and c-Src (in MDA-MB-231 and MDA-MB-235S cells). Stattic increases the apoptotic rate of STAT3-dependent breast cancer cell lines. ^[1]
特徴	Stattic is the first non-peptide small molecule with inhibitory activity against STAT3 SH2 domain regardless of the STAT3 phosphorylation state in vitro.

プロトコル(参考用のみ)

キナーゼアッセイ	High-Throughput Screening and FluorescencePolarization Assays
キナーゼアッセイ	Screening is performed at approximately 30 °C. The specificity ofscreening hits is validated in analogous assays for binding of thetest 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 are: 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 are used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37 °C, proteins are used at 370 nM (STAT3) or 100 nM (Lck). Proteins are incubated with test compounds in Eppendorf tubes at the indicated temperatures for 60 min prior addition of therespective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM).Before measurement at room temperature, the mixtures are allowed to equilibrate for at least 30 min. Test compounds are used at the indicated concentrations diluted from a 20× stock in DMSO. Binding curves and inhibition curves are fitted with SigmaPlot. All competition curves are repeated three times in independent experiment
細胞アッセイ	細胞株	Ly3 cells
	濃度	~2.5 μM
	反応時間	48 h
	実験の流れ	MTS
動物実験	動物モデル	Ly3 parental NOD/SCID IL2R null xenograft
	投薬量	3.75 mg/kg every day
	投与方法	intra tumor

参考

カスタマーフィードバック

: Data from [Data independently produced by FEBS Lett, 2014, 10.1016/j.febslet.2014.11.023]

: Data from [J Biol Chem, 2013, 288(8), 5553-61]

: , , Sci Rep, 2017, 7:41404

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

IL-10 protects against OPC ferroptosis by regulating lipid reactive oxygen species levels post stroke [ Redox Biol, 2024, 69:102982]	PubMed: 38070317
Tumor-associated macrophages drive glycolysis through the IL-8/STAT3/GLUT3 signaling pathway in pancreatic cancer progression [ Cancer Lett, 2024, 588:216784]	PubMed: 38458594
Intracellular CIRP promotes liver regeneration while extracellular CIRP induces ER stress after partial hepatectomy in mice [ Research Square, 2024, 10.21203/rs.3.rs-3840462/v1]	PubMed: none
Macrophage-derived CCL1 targets CCR8 receptor in hepatic stellate cells to promote liver fibrosis through JAk/STAT pathway [ Research Square, 2024, 10.21203/rs.3.rs-3723244/v1]	PubMed: none
Interleukin-13 and its receptor are synaptic proteins involved in plasticity and neuroprotection [ Nat Commun, 2023, 14(1):200]	PubMed: 36639371
Oncogenic KRAS signaling drives evasion of innate immune surveillance in lung adenocarcinoma by activating CD47 [ J Clin Invest, 2023, 133(2)e153470]	PubMed: 36413402
FAM3C/ILEI protein is elevated in psoriatic lesions and triggers psoriasiform hyperproliferation in mice [ EMBO Mol Med, 2023, e16758.]	PubMed: 37226685
LncRNA MALAT1 promotes growth and metastasis of head and neck squamous cell carcinoma by repressing VHL through a non-canonical function of EZH2 [ Cell Death Dis, 2023, 14(2):149]	PubMed: 36813772
Stromal-induced epithelial-mesenchymal transition induces targetable drug resistance in acute lymphoblastic leukemia [ Cell Rep, 2023, 42(7):112804]	PubMed: 37453060
Endothelial Stat3 activation promotes osteoarthritis development [ Cell Prolif, 2023, e13518.]	PubMed: 37309689

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人間や獣医の診断であるか治療的な使用のためにでない。

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