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。
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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。 |
靶点 |
|
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]. |
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 | |
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. |
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 |
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 |