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Unesbulin
CAS No. : 1610964-64-1
MCE 国际站：Unesbulin
产品活性：Unesbulin (PTC596) 是一种口服有效和选择性的 B 细胞特异性莫洛尼氏鼠白血病病毒整合位点 1 (BMI-1) 抑制剂。Unesbulin 在急性髓细胞白血病 (AML) 细胞中可下调 MCL-1 并诱导不依赖 p53 的线粒体凋亡。Unesbulin 具有抗白血病作用。
研究领域：Apoptosis
作用靶点：Apoptosis
In Vitro: Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis.
Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase.
Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1.
Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1.
In Vivo: Unesbulin (PTC596; 5 mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival.
Unesbulin (20 mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells.
Unesbulin (10 or 12.5 mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells.
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