PELI1-EGFR inhibitor S62 is a small molecule inhibitor of the interaction between Pellino-1 (PELI1) and EGFR, suppresses breast cancer metastasis.
PELI1-EGFR inhibitor S62 (5-10 uM) reduced both protein levels of PELI1 and EGFR in MDA-MB-231 cells, also decrease of the membrane EGFR.
PELI1-EGFR inhibitor S62 did not block the phosphorylation of EGFR upon EGF stimulation.
PELI1-EGFR inhibitor S62 reduced the tyrosine and threonine phosphorylation of PELI1 and K63-linked ubiquitination of EGFR.
PELI1-EGFR inhibitor S62 inhibited the metastasis of MDA-MB-231 cells MDA-MB-231 cells-derived tumor nodules in lung after caudal vein injection.
PELI1-EGFR inhibitor S62 is a disruptor of PELI1 and EGFR interaction but not binding to PELI1 or EGFR alone.
Pellino-1 (PELI1) is an E3 ubiquitin ligase acting as a key regulator for the inflammation and autoimmunity via the ubiquitination of the substrate proteins, EGFR is positively correlated with PELI1 expression in breast cancers.