| 产品描述: | EGFR/ErbB1 选择性抑制剂 | 活化剂;EGFR/ErbB1 Selective Inhibitors | Activators;产品介绍:NSC 228155 为 EGFR 激活剂,可与 EGFR 的胞外区域结合,诱导 EGFR 的磷酸化。NSC 228155 是一种有效的 KIX-KID 相互作用抑制剂,能够抑制 CREB 的激酶诱导结构域 (KID) 和 KIX (KID 相互作用结构域,来自 CBP) 的相互作用,IC50 值为 0.36 μM。;InformationNSC228155 is an activator ofEGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.TargetsEGFR ; KIX-KID interaction ; 0.36 μMIn vitroNSC 228155 promotes transactivation of several RTKs, including ErbB2 and ErbB3, Insulin R and IGF-1 R receptors in the cells. It stimulates dimerization of sEGFR domain II. NSC 228155 can rapidly move across cell membranes and disperse within both cytoplasmic and nuclear compartments. It rapidly generates hydrogen peroxide within cells. NSC 228155 is also a potent inhibitor of KIX-KID interaction(IC50 = 0.36 μM), but it is not particularly selective against CREB-mediated gene transcription in HEK 293T cells.Cell Research(from reference)Cell lines:MDA MB468 cells Concentrations:100\u2005μM Incubation Time:15 min |
| 参考文献: |
1. Sakanyan V, et al. 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, et al. 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. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.445 ml |
17.227 ml |
34.453 ml |
| 5 mM |
0.689 ml |
3.445 ml |
6.891 ml |
| 10 mM |
0.345 ml |
1.723 ml |
3.445 ml |
| 50 mM |
0.069 ml |
0.345 ml |
0.689 ml |
|
| 注意: |
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