A BMI1 inhibitor
PTC-028 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.1 It inhibits proliferation of OVCAR-4 and OV-90 ovarian cancer cells (IC50s = ~0.1 ?M for both). It also induces BMI1 degradation in, and apoptosis of, the same cells in a concentration-dependent manner. PTC-028 reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MDS-L myelodysplastic syndrome cells when used at concentrations of 3 and 0.03 ?M, respectively.2 It reduces tumor growth in a OV-90 orthotopic mouse model of ovarian cancer when administered biweekly at a dose of 15 mg/kg.1
1.Dey, A., Xiong, X., Crim, A., et al.Evaluating the mechanism and therapeutic potential of PTC-028, a novel inhibitor of BMI-1 function in ovarian cancerMol. Cancer Ther.17(1)39-49(2018) 2.Zhong, C., Kayamori, K., Koide, S., et al.Efficacy of the novel tubulin polymerization inhibitor PTC-028 for myelodysplastic syndromeCancer Sci.111(12)4336-4347(2020)
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