MYCi975 (NUCC-0200975), an MYCi361 analog, is a novel, orally bioactive and potent MYC inhibitor (Kd = 3.2 μM) with potential anticancer activity. As an improved analog of MYCi361, MYCi975 showed better tolerability. MYCi975 engaged MYC inside cells, disrupted MYC/MAX dimers, and
impaired MYC-driven gene expression. It also enhanced MYC
phosphorylation on threonine-58, consequently increasing
proteasome-mediated MYC degradation. MYCi975 was able to suppresses
tumor growth and enhance anti-PD1 immunotherapy.
纯度:≥98%
CAS:2289691-01-4