STAT3-IN-3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

STAT3-IN-3  纯度: 98.08%

STAT3-IN-3 是一种有效和选择性的 STAT3 抑制剂,有抗增殖活性。STAT3-IN-3 可以引起乳腺癌细胞凋亡 (apoptosis)。STAT3-IN-3 是有前途的靶向线粒体的 STAT3 抑制剂,能用于癌症的研究。

STAT3-IN-3

STAT3-IN-3 Chemical Structure

CAS No. : 2361304-26-7

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STAT3-IN-3 相关产品

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生物活性

STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research[1].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

STAT3-IN-3 has no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2[1].
STAT3-IN-3 inhibits the growth of MDA-MB-231, HCT-116, HepG2, and MCF-7 cells with IC50s of 1.43 μM, 1.89 μM, 2.88 μM, and 3.33 μM, respectively[1].
STAT3-IN-3 down-regulates the expression of STAT3 target genes Bcl-2 and Cyclin D1[1].
STAT3-IN-3 inhibits STAT3 tyrosine phosphorylation and serine phosphorylation[1].
STAT3-IN-3 inhibits STAT3 DNA-binding activity[1].
STAT3-IN-3 (1-4 μM; 24 hours) increases ROS production and remarkably reduces the mitochondrial membrane potential to induce mitochondrial apoptotic pathway[1].
STAT3-IN-3 (1-4 μM; 24 hours) can induce the cleavage of caspase-9, caspase-3 and PARP[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells, HCT-116 cells, HepG2 cells, MCF-7cells
Concentration: MTT assay
Incubation Time: 48 hours
Result: Exhibited anti-proliferative activity.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of MDA-MB-231 cells dose-dependently and the apoptosis rates.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Induced the cleavage of caspase-9, caspase-3 and PARP.

体内研究
(In Vivo)

STAT3-IN-3 (10mg/kg-20 mg/kg; i.p.; daily; for 14 days) possesses potent antitumor activity against implanted 4T1 breast tumors growth[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult female BALB/c mice (6 weeks of age)[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection, daily, for 14 days
Result: Significantly inhibited tumor volume.

分子量

600.48

Formula

C27H26BrN3O6S

CAS 号

2361304-26-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (8.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6653 mL 8.3267 mL 16.6533 mL
5 mM 0.3331 mL 1.6653 mL 3.3307 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Cai G, et al. Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors. Eur J Med Chem. 2019 Jul 15;174:236-251.

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