N-Myc inhibitor N78 is a selective small molecule inhibitor of N-Myc with MST binding Kd of 1.47 uM, 6-fold selective over c-Myc, inhibits viability of MYCN-dependent tumor cells.
N78 markedly inhibits MYCN-Gal4BD luciferase activity at 1 μM, with no effect on CREB-Gal4BD luciferase activity, also not inhibit c-MYC-Gal4BD luciferase activity.
N78 selectively inhibits cells growth of N-Myc expression of N-Myc-dependent neuroblastoma cells.
N78 selectively inhibits N-Myc expression, with greater selectivity and potency than MYCi975, does not effectively suppress c-Myc expression in TNBC cells.
N78 decreases N-Myc protein stability by regulating phosphorylation of N-Myc at threonine 58 (Thr58), leading to subsequent degradation via the proteasome pathway.
N78 (10 mg/kg/d and 20 mg/kg/d) significantly suppressed tumor growth with Tumor growth inhibition (TGI) values of 79.4% and 61.4%, respectively, in neuroblastoma SK-N-BE (2) subcutaneous xenograft model, showing decreased levels of Ki67 and N-Myc in tumor tissues.