产品描述:
PTC-596 is an inhibitor of B cell-specific Moloney murine leukemia virus integration site 1 (BMI1), which is a member of the polycomb repressive complex 1 (PRC1) that has a role in gene silencing.{57574,57575} It inhibits proliferation of MOLM-13 acute myeloid leukemia (AML) and Rec-1 mantle cell lymphoma (MCL) cancer cells (IC50s = 22.4 and 136 nM, respectively). It also induces BMI1 degradation in, and apoptosis of, the same cells. PTC-596 reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MM.1S multiple myeloma cells.{57576} It decreases the number of side population cells, a unique cell population with stem-like characteristics, in Rec-1 cells (IC50 = 138 nM).{57575} PTC-596 (5 mg/kg, p.o.) increases survival in a MOLM-13 mouse xenograft model.{57574}