2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. STAT Ferroptosis Apoptosis Glutathione Peroxidase Bcl-2 Family Reactive Oxygen Species (ROS)
  4. STAT3-IN-51

STAT3-IN-51 是一种 STAT3 抑制剂，可直接与 STAT3 的 SH2 结构域结合。STAT3-IN-51 可诱导细胞凋亡 (apoptosis)、铁死亡 (ferroptosis) 和免疫原性细胞死亡 (ICD)，从而增强抗肿瘤免疫力。STAT3-IN-51 可抑制 STAT3 的激活 (磷酸化，p-STAT3) 及其下游信号传导。STAT3-IN-51 可诱导活性氧 (ROS) 生成，降低 Bcl-2 表达，破坏线粒体功能，抑制 GPX4 活性，并促进脂质过氧化。STAT3-IN-51 可用于结直肠癌、乳腺腺癌、非小细胞肺癌 (NSCLC) 和 Cisplatin (HY-17394) 耐药肺腺癌的研究。

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STAT3-IN-51

STAT3-IN-51 Chemical Structure

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STAT3-IN-51 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

查看 Glutathione Peroxidase 亚型特异性产品:

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GPX1 GPX4

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma[1].

IC50 & Target[1]

STAT3

 

GPX4

 

Bcl-2

 

体外研究
(In Vitro)

STAT3-IN-51 (Compound 8d) (48 小时) 对 SW480，MDA-MB-231，A549 和 A549/DDP 癌细胞系表现出强效的抗增殖活性，其 IC50 值分别为 0.26 μM，0.34 μM，0.61 μM 和 0.67 μM[1]。
STAT3-IN-51 (0.3 μM；24 小时) 通过线粒体功能障碍和半胱天冬酶活化在 SW480 细胞中诱导细胞凋亡[1]。
STAT3-IN-51 (0.3 μM；24 小时) 能有效抑制 SW480 细胞中的总 STAT3 和 p-STAT3 [1]。
STAT3-IN-51 (0.3 μM；24 小时) 促进 CD8+ T 淋巴细胞浸润和增殖[1]。
STAT3-IN-51 (0.3 μM；24 小时) 促进树突状细胞成熟并降低 HMGB1 水平[1]。
STAT3-IN-51 (0.3 μM；24 小时) 通过 GPX4 抑制和脂质过氧化诱导 SW480 细胞的铁死亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

STAT3-IN-51 相关抗体:

Apoptosis Analysis[1]

Cell Line: SW480
Concentration: 0.3 μM
Incubation Time: 24 h
Result: Significantly reduced Bcl-2 expression, increased ROS generation, and induced mitochondrial depolarization. Flow cytometry showed a 8.37% and 30.3% increase in early and late apoptosis in SW480 cells.

Western Blot Analysis[1]

Cell Line: SW480
Concentration: 0.3 μM
Incubation Time: 24 h
Result: Significantly suppressed both total STAT3 and p-STAT3 expression in SW480 cells, demonstrating dual inhibition of STAT3.
Significantly suppressed GPX4 expression.
体内研究
(In Vivo)

STAT3-IN-51 (Compound 8d) (5-10 mg/kg，每两天腹腔注射一次，共 13 天) 在 CT26 肿瘤异种移植模型中显著抑制了肿瘤生长，且安全性良好[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice (5-week-old) bearing CT26 tumor xenografts[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.p. (intraperitoneal); every two days for 13 days
Result: Achieved 63.17% tumor growth inhibition (TGI) at 5 mg/kg, and 75.62% TGI at 10 mg/kg.
At 10 mg/kg, shows better tolerability.
Had minimal toxicity, with no significant histopathological changes or weight loss.
分子量

651.59

Formula

C36H27F6NO4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

STAT3-IN-51 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STAT3-IN-51STATFerroptosisApoptosisGlutathione PeroxidaseBcl-2 FamilyReactive Oxygen Species (ROS)STAT3 inhibitorapoptosisferroptosisimmunogenic cell deathROS generationdecreases Bcl-2 expressiondisruptes mitochondrial functionsuppresses GPX4 activitycolorectal carcinomabreast adenocarcinomanon-small cell lung cancer (NSCLC) and cisplatin-resistant pulmonary adenocarcinomaInhibitorinhibitorinhibit

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