PTC596 is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. PTC596 targets BMI1 expressed by both tumor cells and cancer stem cells (CSCs), and induces hyper-phosphorylation of BMI1, leading to its degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells[1][2].

PTC-209 是一种特异性 BMI-1 抑制剂，HEK293T 细胞系中的 IC50 为 0.5 μM。

PTC-028 can decrease BMI-1 levels by posttranslational modification.