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6-硝基苯并[b] 噻吩-1,1-二氧化物 /Stattic {[allProObj[0].p_purity_real_show]}

货号:A109795 同义名: STAT3 Inhibitor V

Stattic是一种有效的STAT3抑制剂,有效抑制STAT3磷酸化(在Y705和S727)。它还抑制高亲和力磷酸肽与STAT3的SH2结构域的结合,并改善Alport综合征(AS)小鼠的肾功能障碍。

Stattic 化学结构 CAS号:19983-44-9
Stattic 化学结构
CAS号:19983-44-9
Stattic 3D分子结构
CAS号:19983-44-9
Stattic 化学结构 CAS号:19983-44-9
Stattic 3D分子结构 CAS号:19983-44-9
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Stattic 纯度/质量文件 产品仅供科研

货号:A109795 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 STAT1 STAT3 STAT5 其他靶点 纯度
Nifuroxazide 98%
Fludarabine 98%
Artesunate 98%
BP-1-102 +++

STAT3, Kd: 504 nM

99%+
Niclosamide ++

STAT3, IC50: 0.7 μM

98%
Napabucasin 98%
Cryptotanshinone ++

STAT3, IC50: 4.6 μM

98%
Stattic +

STAT3, IC50: 5.1 μM

98%
NSC 74859 +

STAT3, IC50: 86 μM

99%+
Ochromycinone 98%
HO-3867 97%
C188-9 ++++

STAT3, Kd: 4.7 nM

99%+
HJC0152 98%
SH5-07 97%
SH-4-54 ++++

STAT3, Kd: 300 nM

+++

STAT5, Kd: 464 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Stattic 生物活性

靶点
  • STAT3

    STAT3, IC50:5.1 μM

描述 Stattic acts as a potent inhibitor of STAT3 and impedes STAT3 phosphorylation at Y705 and S727 [1]. Stattic hampers the binding of a high-affinity phosphopeptide for the SH2 domain of STAT3 [2]. Stattic improves renal function in Alport syndrome (AS) mice [3].
体内研究

Stattic (10 mg/kg, intraperitoneally, three times per week for 10 weeks) improves renal function in Alport syndrome (AS) mice [3].

体外研究

Stattic (20 μM; 24 hours) inhibits STAT3 phosphorylation at Y705 and selectively inhibits P-STAT3, as evidenced by the lack of inhibition of P-ERK1/2 in ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines [1].

Stattic (2.5, 5, 10 μM; for 4 h) significantly decreases the nuclear levels of pSTAT3 and survivin at 10 μM. Stattic (2.5-10 μM; for 24 h) dose-dependently inhibits IL-6-induced STAT3 activation in PC3M-1E8 cells [2].

Stattic (2.5, 5, 10 μM; for 48 h) suppresses both the growth and induces apoptosis in prostate cancer cells (PC3M-1E8 cells) at 10 μM. However, no significant cell apoptosis is induced with 2.5 μM or 5 μM [2].

Stattic (2.5, 5, 10 μM; for 48 h) results in significant accumulation of cells in the S phase [2].

Stattic does not induce significant morphological changes or apoptosis and exhibits minimal STAT3 phosphorylation in A2780 cells and HUVECs [2].

Stattic 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A431 2 μM Growth Inhibition Assay 2 h blocks EGF-reversed decreases in cell viability 25720435
A431 2 μM Growth Inhibition Assay 2 h increases in apoptosis induced by shikonin 25720435
C13* 0-10 μM Apoptosis Assay 24/48 h induces apoptosis in a dose and time dependent manner 23962558
C13* Apoptosis Assay 24/48 h enhances cisplatin-induced apoptosis 23962558

Stattic 动物研究

Dose Mice: 10 mg/kg[3] (i.p.), 1 mg/kg[4] (i.p.); 10 mg/kg[5] (s.c.); 50 mg/kg[6] (p.o.)
Administration i.p., s.c., p.o.

Stattic 参考文献

[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.

Stattic 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.73mL

0.95mL

0.47mL

23.67mL

4.73mL

2.37mL

47.35mL

9.47mL

4.73mL

Stattic 技术信息

CAS号19983-44-9
分子式C8H5NO4S
分子量 211.195
别名 STAT3 Inhibitor V
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(236.75 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

5% DMSO+40% PEG 300+5% Tween 80+50% water 10 mg/mL

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