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。
| 生物活性 | STAT3-IN-3 is a potent and selective inhibitor ofsignal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 inducesapoptosisin breastcancercells. STAT3-IN-3 acts as a promising mitochondria-targetingSTAT3 inhibitorforcancerresearch[1]. |
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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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(8.33 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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