Dibenzazepine (YO-01027)

InformationDibenzazepine (YO-01027, DBZ) is a dipeptidicγ-secretaseinhibitor withIC50of 2.6 nM and 2.9 nM in cell-free assays forAPPLandNotchcleavage, respectively.In vitroYO-01027 interacts directly with theγ-secretase complex and targets the N-terminal Presenilin fragment. Increasing concentrations of YO-01027 administered to APPL- or Notch-expressing cells leads to the progressive accumulation of APPL CTF fragments and a decrease in NICD production in a strictly dose-dependent manner. 10 μM of YO-01027 reduces breast cancer stem cells (BCSC) number and activity. A recent research indicates YO-01027 impairs mucin protein MUC16 biosynthesis in a concentration-dependent manner in undifferentiated cells at both preconfluent and confluent stages through Notch inhibition, but not in postmitotic stratified cells.In vivoYO-01027, which is delivered 1 mg/mL by i.p. injection on the day of cell injection and every subsequent 3 days, YO-01027 significantly, decreases MCF7 but not MDA-MB-231 tumors and increases latency compared with control mice (18-28 days). YO-01027-treated MCF7 tumors that did form had significantly reduced tumor volumes. Treatment of YO-01027 into C57BL/6 mice inhibits epithelial cell proliferation and induces goblet cell differentiation in intestinal adenomas in a dose-dependent manner.Cell Datacell lines：Concentrations：10 μMIncubation Time：3 daysPowder Purity:≥97%.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C26H23F2N3O3

Molecular Weight: 463.48