Dibenzazepine (YO-01027)

For research use only.

Catalog No.S2711

20 publications

Dibenzazepine (YO-01027) Chemical Structure

Molecular Weight(MW): 463.48

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.

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Selleck's Dibenzazepine (YO-01027) has been cited by 20 publications

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Biological Activity

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.
Targets
γ secretase(APPL) [1]
(Cell-free assay)
γ secretase(Notch) [1]
(Cell-free assay)
2.6 nM 2.9 nM
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. [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]

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. [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]

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[2]

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  • Cell lines: BCSC
  • Concentrations: 10 μM
  • Incubation Time: 3 days
  • Method:

    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)
Animal Research:

[4]

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  • Animal Models: C57BL/6 mice
  • Dosages: 0, 3, 10, 30 μmol/kg
  • Administration: Injected daily intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (198.49 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose
For best results, use promptly after mixing.
6 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 463.48
Formula

C26H23F2N3O3

CAS No. 209984-56-5
Storage powder
in solvent
Synonyms N/A
Smiles CC(NC(=O)CC1=CC(=CC(=C1)F)F)C(=O)NC2C(=O)N(C)C3=C(C=CC=C3)C4=C2C=CC=C4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    How to dissolve the compund for in vivo applications?

  • Answer:

    For S2711, we suggest to use 0.5% hydroxyethyl cellulose in vivo study.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID