10058-F4 is a specific c-Myc inhibitor that disrupts the association between the c-Myc and Max, inhibits HL60 cell growth with IC50 of 51 uM.
10058-F4 arrests AML cells at G0/G1 phase, downregulates c-Myc expression and upregulates CDK inhibitors p21 and p27.
10058-F4 induces apoptosis through activation of mitochondrial pathway shown by downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, and cleavage of caspase 3, 7, and 9.
10058-F4 also induces myeloid differentiation.
