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CAS No.: 2059952-75-7

STAT3-IN-1 Catalog No. CSN27227

Synonyms: STAT3-IN-7d

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 .

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1029 mL
- 10.5145 mL
- 21.0290 mL
- 5 mM
- 0.4206 mL
- 2.1029 mL
- 4.2058 mL
- 10 mM
- 0.2103 mL
- 1.0515 mL
- 2.1029 mL

技术信息

CAS号

2059952-75-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H29NO6

运输

蓝冰

分子量

475.53

别名

STAT3-IN-7d

溶解度

DMSO	95.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (10.5 mM)

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