2. JAK/STAT Signaling Stem Cell/Wnt NF-κB Apoptosis
  3. STAT NF-κB Apoptosis Caspase Bcl-2 Family
  4. STAT3/NF-κB-IN-1

STAT3/NF-κB-IN-1 是一种强效的 STAT3 和 NF-κB 抑制剂，其在 4 T1 细胞中的 IC50 值分别为 5.86 (STAT3) 和 4.22 μM (NF-κB)。STAT3/NF-κB-IN-1 能够通过上调关键的凋亡调节因子 (caspases-3、9、Bax) 以及下调 Bcl-2 的表达来诱导细胞凋亡 (apoptosis)。STAT3/NF-κB-IN-1 对乳腺癌细胞系具有显著的抗癌活性，并能在体内减少肿瘤体积。STAT3/NF-κB-IN-1 可用于乳腺癌的研究。

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STAT3/NF-κB-IN-1

STAT3/NF-κB-IN-1 Chemical Structure

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STAT3/NF-κB-IN-1 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STAT3/NF-κB-IN-1 is a potentSTAT3 and NF-κB inhibitor with IC50s of 5.86 (STAT3) and 4.22 μM (NF-κB) in 4 T1 cells. STAT3/NF-κB-IN-1 is able to induce apoptosis via its upregulation on key apoptotic regulators; caspases-3,9, Bax and downregulation of Bcl-2. STAT3/NF-κB-IN-1 exerts considerable anticancer activity against breast cancer cell lines and reduces tumor volume in vivo. STAT3/NF-κB-IN-1 can be used for the study of breast cancer[1].

IC50 & Target[1]

NF-κB

4.22 μM (IC50)

STAT3

5.86 μM (IC50)

Caspase-3

 

Caspase-9

 

Bcl-2

 

Bax

 

体外研究
(In Vitro)

STAT3/NF-κB-IN-1 (Compound 12a) (72 h) 对 4T1、MDA-MB-231、MDA-MB-468 和 MCF-7 细胞具有细胞毒性，其 IC50值分别为 7.68、1.53、7.00 和 6.14μM[1]。
STAT3/NF-κB-IN-1 (10 μM, 24 h) 显著抑制 4T1 和 MDA-MB-231 细胞的迁移和侵袭[1]。
STAT3/NF-κB-IN-1 (1-10 μM, 24-72 h) 显著诱导 MDA-MB-231 细胞早期凋亡，同时激活 caspase 3/9 和增加Bax/Bcl-2[1]。
STAT3/NF-κB-IN-1 (1-5 μM, 48-96 h) 显著抑制 p-STAT3 和 NF-κB 的表达[1]。

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

STAT3/NF-κB-IN-1 相关抗体:

Cell Migration Assay [1]

Cell Line: 4T1 and MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Showed the percentage of scratch closure corresponding to cell migration of 15%.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 1, 2.8, 6 and 10 μM
Incubation Time: 24, 48 and 72 h
Result: Considerably raised the % of apoptotic cells positive to annexin V FITC.
Increased early (ranging from 0.55 % to 22.51 %) and late apoptosis (ranging from 0.18 % to 16.07 %).
Had dose-dependent (1, 2.8 and 6 μM for 48 h) and time dependent (2.8 μM for 24, 48 and 72 h) effects on caspase-9 expression.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 1.5, 2 and 5 μM
Incubation Time: 48, 72 and 96 h
Result: Inhibited the phosphorylation of p-STAT3 Y705 protein as well as slightly downregulate the expression level of total STAT3.
Clearly suppressed NF-κB protein levels.
Had dose-dependent (1, 2 and 5 μM for 72 h) and time-dependent effects (2 μM for 48, 72 and 96 h) p-SAT3 and NF-kB expression.
体内研究
(In Vivo)

STAT3/NF-κB-IN-1 (Compound 12a) (40 mg/kg, s.c. 每天一次共 12 天) 在小鼠埃利希氏腹水癌模型中具有显著的抗肿瘤活性[1]。

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

Animal Model: Ehrlich solid carcinoma model established in BALB/c mice[1]
Dosage: 40 mg/kg
Administration: Subcutaneous injection (s.c.), once daily for 12 days
Result: Decreased the tumor volume by 70-80%, and there was no significant toxicity.
分子量

542.61

Formula

C27H26N8O3S
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/NF-κB-IN-1 相关分类

  • 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 *
= × ×

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.

Keywords:

STAT3/NF-κB-IN-1STATNF-κBApoptosisCaspaseBcl-2 FamilyNuclear factor-κBNuclear factor-kappaBBreast CancerPurineTheophyllineInhibitorinhibitorinhibit

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