NCIt synonyms : Polycomb Ring Finger Oncogene Inhibitor PTC596;
NCIt definition : An orally active inhibitor of the polycomb ring finger oncogene BMI1 (B-cell-specific
Moloney murine leukemia virus integration site 1), with potential antineoplastic activity.
Upon oral administration, unesbulin targets BMI1 expressed by both tumor cells and
cancer stem cells (CSCs), and induces hyper-phosphorylation of BMI1 leading to its
degradation. This inhibits BMI1-mediated signal transduction pathways and results
in a reduction of proliferation of BMI1-expressing tumor cells. BMI1, a key protein
in the polycomb repressive complex 1 (PRC1), is overexpressed in certain tumor cell
types, and plays a key role in CSC survival, proliferation and resistance to chemotherapeutics;
its expression is associated with increased tumor aggressiveness and a poor prognosis.;
UNII : Z4HZ70S62Q;
InChIKey : TWLWOOPCEXYVBE-UHFFFAOYSA-N;
CAS number : 1610964-64-1; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1610964-64-1
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