产品信息
抗原名称
γ secretase(APPL) ,γ secretase(Notch)
商品描述
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively.
分子量
463.48
纯度
>98%
可溶性
DMSO : 50 mg/mL (107.88 mM; Need ultrasonic)
外观
white to beige Powder
In vitro(体外研究)
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(体内研究)
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.
背景
别名
二苯并氮卓
分子式
C26H23F2N3O3
CAS号
209984-56-5
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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