NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

KIX-KID:0.36 μM

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)