A cell-permeable indandione compound that inhibits the Bmi1-Ring1A E3 complex ubiquitin ligase activity both in cell-free assays (by 100% against self- and Top2alpha ubiquitination at 25 and 50uM, respectively) and in HeLa cells (by 100% against Bmi1 ubiquitination at 50uM). Shown to greatly potentiate Teniposide (VM26) cancer cytotoxicity (by 10-fold in A375 and A549 cultures at 5.5 and 33uM, respectively) by preventing Top2alpha degradation following VM26 treatment (100% inhibition at 50uM in HeLa cells).
Solubility:DMSO
Primary Target:BMI1/RING1A
Molar Mass:235.2
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
