NSC228155 是一种 EGFR 的激活剂，与 sEGFR 二聚化结构域 II 结合并调节 EGFR 酪氨酸磷酸化。

NSC228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation.

NSC 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[1]. NSC 228155 can rapidly move across cell membranes and disperse within both cytoplasmic and nuclear compartments. It rapidly generates hydrogen peroxide within cells[2]. 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[3].

MDA MB468 cells serum-starved overnight are pre-incubated (or not) with 10?μM AG1478 or 2?μM PD 153035 for 90?min and then, where indicated, incubated with 100?μM NSC 228155 or CN 009543V or 150?ng/ml EGF or vehicle (0.2% DMSO) for 15?min. Proteins are blotted to nitrocellulose membrane and analyzed with biotinylated anti-pTyr P100, anti-pEGFR Y1068 and anti-EGFR (epitope in cytoplasmic region) antibodies. (Only for Reference)

113104-25-9

C11H6N4O4S

290.25

NSC228155

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:12 mg/mL (41.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years