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STAT3-IN-1 {[allProObj[0].p_purity_real_show]}

货号:A1176397

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis .

STAT3-IN-1 化学结构 CAS号:2059952-75-7
STAT3-IN-1 化学结构
CAS号:2059952-75-7
STAT3-IN-1 3D分子结构
CAS号:2059952-75-7
STAT3-IN-1 化学结构 CAS号:2059952-75-7
STAT3-IN-1 3D分子结构 CAS号:2059952-75-7
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STAT3-IN-1 纯度/质量文件 产品仅供科研

货号:A1176397 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。

STAT3-IN-1 生物活性

描述 Signal transducer and activator of transcription 3 (STAT3) is a cytoplasmic protein that plays important roles in oncogenic signaling pathways. STAT3-IN-1 (compound 7d) is a potent, selective and orally active STAT3 inhibitor with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. Exposing MDA-MB-231 cells to STAT3-IN-1 (1-5 μM) for 48 h led to dose-dependent inhibition of STAT3 acetylation at Lys685 residue. STAT3-IN-1 increased the expressions of the tumor-suppressor genes which were related to STAT3 acetylation at Lys685, thereby further demonstrated that STAT3-IN-1 inhibited STAT3 acetylation. In MDA-MB-231 cancer cells, STAT3-IN-1 (1-5 μM for 48 hr) markedly decreased the phospho-Tyr705 STAT3 in a dose-dependent manner without affecting the total STAT3, indicating that STAT3-IN-1 selectively decreased the level of p-STAT3. STAT3-IN-1 (1-10 μM for 48 hr) dose-dependently inhibited the proliferation of STAT3 dependent MDA-MB-231 cells. STAT3-IN-1 (10 mg/kg, 20 mg/kg) significantly inhibited tumor growth as reflected in decreased tumor weight. And the level of p-STAT3 (Y705) was also inhibited in tumor tissues from mice treated with STAT3-IN-1[2].

STAT3-IN-1 参考文献

[1]Li S, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein. Eur J Med Chem. 2016 Nov 29;124:1006-1018.

[2]Li S, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein. Eur J Med Chem. 2016 Nov 29;124:1006-1018

STAT3-IN-1 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.51mL

2.10mL

1.05mL

21.03mL

4.21mL

2.10mL

STAT3-IN-1 技术信息

CAS号2059952-75-7
分子式C28H29NO6
分子量 475.533
别名
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,Room Temperature

溶解度

DMSO: 120 mg/mL(252.35 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
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