Unesbulin, also known as 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. 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. It decreases the number of side population cells, a unique cell population with stem-like characteristics, in Rec-1 cells (IC50 = 138 nM). PTC-596 (5 mg/kg, p.o.) increases survival in a MOLM-13 mouse xenograft model.
MedKoo Cat#: 206519
Name: Unesbulin HCl
CAS#: Unesbulin HCl
Chemical Formula: C19H14ClF5N6
Exact Mass:
Molecular Weight: 456.80
Elemental Analysis: C, 49.96; H, 3.09; Cl, 7.76; F, 20.79; N, 18.40
The following data is based on the product molecular weight 456.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
