|2-((7-硝基苯并[c][1,2,5]恶二唑-4-基)硫基)吡啶 1-氧化物|CsnPharm

CAS No.: 113104-25-9

NSC 228155 Catalog No. CSN22616

Synonyms: NSC-228155

NSC228155 can enhance the tyrosine phosphorylation of EGFR via binding to the dimerization domain II. It blocks KIX-KID interaction as well (IC50 = 0.36 μM).

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400-920-2911

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技术信息

生物活性

描述Ligand-dependent activation of epidermal growth factor receptor (EGFR) is an essential process governing signal transduction during cell growth, differentiation, survival, and proliferation in physiological conditions. Mutations resulting in overexpression or deregulation of the receptor impair signal transduction, leading to tumor growth. NSC-228155 is an activator of EGFR, which has a positive log P and could enter cells and enhance EGFR tyrosine phosphorylation ^[1]. It also dose-dependently inhibits KIX-KID interaction with an IC₅₀ of 0.36 μM ^[2]. The increase in the fluorescence curve at 665 nm was moderately suppressed in the cells exposed to NSC-228155 indicating the generation of H₂O₂ in redox cycling, which could activate EGFR. NSC-228155 provided high yields of stable SOD1 (superoxide dismutase 1) dimer at concentration of 100 μM for 15 min in MDA MB468 cells, suggesting specific action of NSC-228155 on SOD1. Further studies showed that EGFR tyrosine phosphorylation was enhanced through the action of SOD1 dimer shortly after exposure of cells to 100 μM NSC-228155 for 10 min. Taken together, NSC-228155 primarily induced the formation of a stable SOD1 dimer that was functionally active and led to the accumulation of intracellular H₂O₂, which in turn activates EGFR ^[1].
参考文献

[1] Sakanyan V. Activation of EGFR by small compounds through coupling the generation of hydrogen peroxide to stable dimerization of Cu/Zn SOD1. Sci Rep. 2016 Feb 17;6:21088.
[2] Xie F. Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5371-5. doi: 10.1016/j.bmcl.2013.07.053. Epub 2013 Jul 31.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4452 mL
- 17.2262 mL
- 34.4525 mL
- 5 mM
- 0.6890 mL
- 3.4452 mL
- 6.8905 mL
- 10 mM
- 0.3445 mL
- 1.7226 mL
- 3.4452 mL

技术信息

CAS号

113104-25-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H6N4O4S

运输

蓝冰

分子量

290.25

别名

NSC-228155

溶解度

DMSO	27.0 mg/mL (93.0 mM) warming
Water	insoluble

动物实验配方

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