SK2188 is a potent and selective PROTAC degrader targeting AURKA (DC50 = 3.9 nM). It induces DNA damage and apoptosis (Apoptosis), indirectly degrades MYCN, and inhibits tumor cell proliferation, offering insights for research on MYCN-amplified neuroblastoma.

SK2188 is effective at inhibiting proliferation in MYCN-amplified cells at concentrations of 10-10000 nM over 48-120 hours, and it is also effective on patient-derived organoid cells. In NGP cells, SK2188 at 10-1000 nM for 24 hours suppresses cell growth by inducing apoptosis. Additionally, SK2188 at 10-1000 nM over 1-72 hours leads to AURKA degradation, causing DNA damage and replication stress in NGP cells. Furthermore, SK2188 at concentrations of 100-1000 nM for 3 hours demonstrates high target selectivity and degradation specificity in NGP cells.