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。

Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.

Solid

BMI-1

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Nishida Y, et al. The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells. Blood Cancer J. 2017 Feb 17;7(2):e527.
[2]. BMI1 inhibitor PTC596

In Vitro: DMSO : 16.67 mg/mL (39.66 mM; Need ultrasonic)配制储备液