For research use only.
CAS No. 209984-56-5
Dibenzazepine (YO-01027) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.
Selleck's Dibenzazepine (YO-01027) has been cited by 25 publications
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Choose Selective Gamma-secretase Inhibitors
|Description||Dibenzazepine (YO-01027) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.|
YO-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 vivo||YO-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. |
Pharmacological Inhibition of γ-secretase Activity:For YO-01027, pilot experiments are performed with different drug concentrations ranging from 0.1 nM to 250 nM to determine the effective linear range and maximal inhibition dose for YO-01027. YO-01027 is added at the required concentrations to the S2 cell medium upon induction of Notch or APPL expression, 6 hours before protein harvesting. For each sample, YO-01027 is also included at the corresponding concentration in the lysis buffer for protein extraction and immunoblot analysis.
|In vitro||DMSO||92 mg/mL (198.49 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose
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