1. MAPK/ERK Pathway Cell Cycle/DNA Damage Apoptosis Autophagy Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Ribosomal S6 Kinase (RSK) Topoisomerase Apoptosis Autophagy Reactive Oxygen Species (ROS)
  3. RSK2/TOP2-IN-1

RSK2/TOP2-IN-1 是一种 RSK2/TOP2 双重抑制剂。RSK2/TOP2-IN-1 靶向关键的肿瘤进展酶,包括核糖体 S6 激酶 (ribosomal S6 kinase) 2 和拓扑异构酶 (topoisomerases) IIα/IIβ。RSK2/TOP2-IN-1 对所有鳞状细胞癌 (SCC) 细胞系的选择性指数均大于 2。RSK2/TOP2-IN-1 可诱导细胞凋亡 (apoptosis)、自噬 (autophagy) 和活性氧 (ROS) 的产生。RSK2/TOP2-IN-1 可用于癌症研究,如鳞状细胞癌。

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RSK2/TOP2-IN-1

RSK2/TOP2-IN-1 Chemical Structure

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查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma[1].

IC50 & Target[1]

RSK2

 

topoisomerase II alpha

 

topoisomerase II beta

 

体外研究
(In Vitro)

RSK2/TOP2-IN-1 (Compound 7e) (72 h) 对口腔鳞状细胞癌 (SCC-4、SCC-9、SCC-25) 细胞具有强效细胞毒性,其 IC50 值分别为 57.1、46.5 和 13.0 μM[1]
RSK2/TOP2-IN-1 (72 h) 可抑制结直肠癌 HCT-116 细胞、肝癌 HepG2 细胞和黑色素瘤 B16-F10 细胞, IC50 值分别为 9.1、3.4 和 7.5 μM[1]
RSK2/TOP2-IN-1 (500 μM, 24 h) 对红细胞的溶血率小于 2%[1]
RSK2/TOP2-IN-1 (93 μM, 24 h) 可诱导 SCC-9 细胞凋亡[1]
RSK2/TOP2-IN-1 (46.5 μM, 48 h) 可诱导 SCC-9-LC3-GFP 细胞中 LC3 阳性自噬小体的形成[1]
RSK2/TOP2-IN-1 (93 μM, 24-72 h) 会诱导 SCC-9 细胞中活性氧的产生[1]
RSK2/TOP2-IN-1 (2.91 μM, 72 h) 能抑制 SCC-9 细胞的迁移,伤口闭合率为 54.7%[1]

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

Apoptosis Analysis[1]

Cell Line: SCC-9 cells
Concentration: 93 μM
Incubation Time: 24 h
Result: Activated caspase 3/7 with 78.6% positive cells.
Induced cell shrinkage and membrane blebbing.
体内研究
(In Vivo)

RSK2/TOP2-IN-1 (Compound 7e) (100-400 mg/kg,腹腔注射,单次给药) 在 C57BL/6 小鼠中未导致死亡,也未导致体重下降[1]

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

Animal Model: C57BL/6 mice[1]
Dosage: 100, 200 and 400 mg/kg
Administration: Intraperitoneally injection
Result: Caused no death and no body weight loss.
Had no lesions in liver, kidney, heart, or other organs in necropsy.
Had a predicted median lethal dose of 2000 mg/kg.
分子量

518.64

Formula

C29H26O5S2

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

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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:
RSK2/TOP2-IN-1
目录号:
HY-178029
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