aladdin 阿拉丁 Y129283 YO-01027,γ分泌酶抑制剂 209984-56-5 ≥97%

中文名：Dibenzazepine (YO-01027)

英文名：Dibenzazepine (YO-01027)

纯度：10mM in DMSO

货号：D408731

Cas号：209984-56-5

存储温度：-80℃储存

运输条件：特低温运输

产品介绍：

Information

Dibenzazepine (YO-01027, DBZ) is a dipeptidicγ-secretaseinhibitor withIC50of 2.6 nM and 2.9 nM in cell-free assays forAPPLandNotchcleavage, respectively.
In vitro

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.
Cell Data

cell lines：

Concentrations：10 μM

Incubation Time：3 days

Powder Purity:≥97%

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