NSC 228155

产品说明书

Print
Chemical Structure| 113104-25-9 同义名 : -
CAS号 : 113104-25-9
货号 : A608208
分子式 : C11H6N4O4S
纯度 : 99%
分子量 : 290.255
MDL号 : MFCD30742994
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(51.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.45mL

0.69mL

0.34mL

17.23mL

3.45mL

1.72mL

34.45mL

6.89mL

3.45mL
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.