1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Immunology/Inflammation Protein Tyrosine Kinase/RTK Epigenetics
  2. STAT c-Myc Bcl-2 Family Interleukin Related JAK
  3. STAT3-IN-46

STAT3-IN-46 是一种选择性且具有口服活性的信号转导和转录激活因子 3 (STAT3) 抑制剂,KD 值为 323.3 nM。STAT3-IN-46 直接与 STAT3 的 SH2 结构域结合,抑制 IL-6/JAK/STAT3 信号通路(IC50 值为 0.87 μM),并下调 c-MycBcl-2 的水平。STAT3-IN-46 可用于癌症研究,例如三阴性乳腺癌。

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STAT3-IN-46

STAT3-IN-46 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STAT3-IN-46 is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) (KD = 323.3 nM). STAT3-IN-46 directly binds to the SH2 domain of the STAT3 and inhibits IL-6/JAK/STAT3 signaling pathway (IC50 = 0.87 μM) and downregulates c-Myc and Bcl-2 levels. STAT3-IN-46 can be used for the research of cancer, such as triple-negative breast cancer[1].

IC50 & Target[1]

STAT3

323.3 nM (Kd)

Bcl-2

 

IL-6

 

体外研究
(In Vitro)

STAT3-IN-46 (Compound W36) 在 MDA-MB-231 和 MDA-MB-468 细胞中显示出抗增殖活性,其 IC50 值分别为 0.61 和 0.65 μM[1]
STAT3-IN-46 在 HEK293 和 HK2 细胞中显示出最小的细胞毒性作用,其 IC50 值分别为 1.87 和 1.73 μM[1]
STAT3-IN-46 在 HEK-Blue-IL-6 细胞中抑制 IL-6/JAK/STAT3 信号通路,IC50 值为 0.87 μM[1]
STAT3-IN-46 (2.5-10 μM, 6-12 h) 抑制 MDA-MB-231 和 MDA-MB-468 细胞中磷酸化 STAT3 的水平[1]
STAT3-IN-46 (2.5-10 μM, 24 h) 可下调 MDA-MB-231 和 MDA-MB-468 细胞中 c-MycBcl-2 的水平[1]

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

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and MDA-MB-468 cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 6, 12 and 24 h
Result: Reduced p-STAT3 levels.
Did not affect STAT1 and STAT5 phosphorylation levels.
Downregulated c-Myc and Bcl-2 levels.
体内研究
(In Vivo)

STAT3-IN-46 (Compound W36) (腹腔注射 7.5-10 mg/kg 或口服 100 mg/kg,每日一次,持续 16 天) 可抑制 MDA-MB-231 异种移植小鼠模型中的肿瘤生长[1]

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

Animal Model: MDA-MB-231 xenograft mice models[1]
Dosage: 7.5 and 10 mg/kg (Intraperitoneally injection) and 100 mg/kg (Orally administration)
Administration: Daily for 16 days
Result: Reduced tumor volume.
Had no body weight loss.
分子量

564.68

Formula

C31H29FN8S

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
STAT3-IN-46
目录号:
HY-175771
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