Powder: -20°C for 3 years | In solvent: -80°C for 1 year
YO-01027 (DBZ) 是一种高效的 γ-分泌酶抑制剂,能够裂解 Notch (IC50:2.92 nM) 和 APPL (IC50:2.64 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 435 | 现货 | ||
2 mg | ¥ 595 | 现货 | ||
5 mg | ¥ 813 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,430 | 现货 | ||
50 mg | ¥ 3,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 829 | 现货 |
产品描述 | YO-01027 (DBZ) is a potent γ-secretase inhibitor. |
靶点活性 | γ-secretase (Notch):2.9 nM, γ-secretase (APPL):2.6 nM |
体外活性 | 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. [1] 10 μM of YO-01027 reduces breast cancer stem cells (BCSC) number and activity. [2] 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. [3] |
体内活性 | 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. [2] 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. [4] |
激酶实验 | 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. |
细胞实验 | Cells are resuspended at ≤1 × 106 in 100 μL sorting buffer (PBS containing 0.5% bovine serum albumin, 2 mM EDTA) and incubated with preconjugated primary antibodies BEREP4-FITC (1:10), CD44-APC (1:20), and CD24-PE (1:10) for 10 minutes at 4 °C. The cells are washed in PBS and centrifuged at 800 × g for 2 minutes. For analysis, cells are resuspended in 500 μL of sorting buffer and fluorescence is measured using FACSCalibur and analyzed using WinMIDI 2.8. For sorting, cells are resuspended in 1× HBSS after incubation with the primary antibodies. Cells are sorted, with HBSS as sheath fluid, at 16 p.s.i. using FACSAria. The CD24low cell population gated by FACS is the lowest quintile of CD24-positive cells plus all the CD24-negative cells.(Only for Reference) |
别名 | gamma-Secretase Inhibitor XX, Dibenzazepine, DBZ, 二苯并氮卓 |
分子量 | 463.48 |
分子式 | C26H23F2N3O3 |
CAS No. | 209984-56-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 46.4 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1576 mL | 10.788 mL | 21.5759 mL | 53.9398 mL |
5 mM | 0.4315 mL | 2.1576 mL | 4.3152 mL | 10.788 mL | |
10 mM | 0.2158 mL | 1.0788 mL | 2.1576 mL | 5.394 mL | |
20 mM | 0.1079 mL | 0.5394 mL | 1.0788 mL | 2.697 mL | |
50 mM | 0.0432 mL | 0.2158 mL | 0.4315 mL | 1.0788 mL | |
100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5394 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
YO-01027 209984-56-5 Neuroscience Proteases/Proteasome Stem Cells Gamma-secretase γ-secretase Gamma secretase Notch gamma-Secretase Inhibitor XX YO01027 inhibit Dibenzazepine YO 01027 DBZ Inhibitor 二苯并氮卓 inhibitor