| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | 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[1]. Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase[1]. Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1[1]. Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1[2]. Apoptosis Analysis[1] Cell Line: | ||||||||||||
| Name | Unesbulin | ||||||||||||
| CAS | 1610964-64-1 | ||||||||||||
| Formula | C19H13F5N6 | ||||||||||||
| Molar Mass | 420.34 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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