1. PI3K/Akt/mTOR NF-κB Apoptosis
  2. PI3K Akt NF-κB Bcl-2 Family Apoptosis
  3. Nogo-B-IN-1

Nogo-B-IN-1 ((S,R)-4v) 是一种共价 Nogo-B 抑制剂。Nogo-B-IN-1 通过抑制 Nogo-B 活性和 PI3K/AKT/NF-κB/Bcl-2 信号通路来抑制骨肉瘤 (OS) 的进展。Nogo-B-IN-1 抑制 OS 143B 细胞的增殖 (IC50 =0.28 µM),诱导细胞凋亡 (apoptosis)。Nogo-B-IN-1 可用于 OS 靶向研究。

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Nogo-B-IN-1

Nogo-B-IN-1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nogo-B-IN-1 ((S,R)-4v) is a covalent Nogo-B inhibitor. Nogo-B-IN-1 inhibits the progression of osteosarcoma (OS) by suppressing Nogo-B activity and the PI3K/AKT/NF-κB/Bcl-2 signaling pathway. Nogo-B-IN-1 inhibits the proliferation of OS 143B cells (IC50 = 0.28 µM) and induces apoptosis. Nogo-B-IN-1 can be used for OS targeting research[1].

体外研究
(In Vitro)

Nogo-B-IN-1 (0-3 μM, 24 小时) 在 143B 细胞中依赖 Nogo-B 来抑制细胞迁移和增殖,诱导细胞形态异常、细胞收缩、排列紊乱,导致细胞凋亡[1]
Nogo-B-IN-1 (50 μM) 可抑制 Nogo-B 表达,在 143B 细胞中的抑制活性为 99%[1]
Nogo-B-IN-1 (0-3 μM, 24 小时) 可抑制 Nogo-B,进而削弱 143B 细胞中的 PI3K/AKT 和 NF-κB 活性[1]

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

Cell Migration Assay [1]

Cell Line: 143B cells
Concentration: 0 nM, 300 nM, 1000 nM
Incubation Time: 24 h
Result: Decreased the percentage of intercellular wound healing distance, decreased the colony growth.

Apoptosis Analysis[1]

Cell Line: 143B cells
Concentration: 0 nM, 300 nM, 1000 nM
Incubation Time: 24 h
Result: Induced apoptosis.

Western Blot Analysis[1]

Cell Line: 143B cells
Concentration: 0, 0.3, 0.5, 1, 3 μM
Incubation Time: 0, 24, 48, 72 h
Result: Downregulated Nogo-B protein level, enhanced the stability of Nogo-B.
Decreased p65, Bcl-2 protein, inhibited activation of PI3K, AKT, and p-AKT.

RT-PCR[1]

Cell Line: 143B cells
Concentration: 0, 0.3, 0.5, 1, 3 μM
Incubation Time: 24 h
Result: Had no effect of Nogo-B mRNA level.
体内研究
(In Vivo)

Nogo-B-IN-1 (30 mg/kg,腹腔注射,每日一次,23 天) 在 143B 异种移植 BALB/c 裸鼠模型中抑制 OS 进展,且无明显毒性[1]
Nogo-B-IN-1 (30 mg/kg,腹腔注射,每日一次,23 天) 在 43B Nogo-B 敲低异种移植 BALB/c 裸鼠模型中减弱了肿瘤体积和肿瘤重量的抑制作用[1]

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

Animal Model: 143B (5 ×106) xenograft BALB/c nude mice (3-month-old) model[1]
Dosage: 30 mg/kg
Administration: i.p., once a day, 23 days
Result: Suppressed tumor growth, had no discernible morphological changes in the heart, liver, spleen, or kidney tissues.
Animal Model: 143B (5 ×106) with Nogo-B knockdown xenograft BALB/c nude mice (3-month-old) model[1]
Dosage: 30 mg/kg
Administration: i.p., once a day, 23 days
Result: Was weakened the inhibitory effect of tumor volume and tumor weight.
分子量

605.89

Formula

C29H27Cl3N2O6

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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