MYCi361 (NUCC-0196361) is a small molecule MYC inhibitor, binds to MYC protein with KD of 3.2 uM, disrupts MYC/MAX complex formation.
MYCi361 impaired MYC/MAX heterodimer but not the closely related MAX/MAX homodimer binding to E-box DNA.
MYCi361 disrupts the MYC/MAX interaction in PC3 cells at concentration 6 μM for 1 hr.
MYCi361 decreases MYC protein stability by modulating MYC-threonine 58 phosphorylation.
MYCi361 inhibits cell proliferatin ona panel of MYC-dependent and -independent cell lines (LNCaP cell IC50 =1.4 uM, MV411, IC50=2.6 uM).
MYCi361 shows favorable pharmacokinetics and inhibits MYC-driven tumor growth in vivo.
MYCi361 modulates the tumor immune microenvironment and enhances anti-PD1 immunotherapy.
