YO-01027 (Dibenzazepine, DBZ)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    YO-01027, also known as dibenzazepine or DBZ, is a potent inhibitor of γ-secretase, a multisubunit aspartyl protease catalyzing the cleavage of numerous type I integral membrane proteins (such as amyloid precursor protein (APP) and Notch). YO-01027 also potently blocks amyloid precursor protein-like (APPL) and Notch cleavage, with estimated inhibition constant IC50 of 2.640.30 nM and 2.920.22 nM respectively, through interaction with the N-terminal fragment of Presenilin in a dose-response manner. Recent studies show that YO-01027-induced inhibition Notch signaling pathway leads to a rapid conversion of proliferative crypt cells into postmitotic cells and impairs MUC16 biosynthesis in a concentration-dependent manner in undifferentiated cells instead of postmiotic stratified cells at both preconfluent and confluent stages.
- Properties
  - Alternative Name
    
    gamma-Secretase Inhibitor XX,YO01027; (2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide
    
    CAS Number
    
    209984-56-5
    
    Molecular Formula
    
    C26H23F2N3O3
    
    Molecular Weight
    
    463.48
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥23.17 mg/mL in DMSO; insoluble in H2O; ≥4.13 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yu-Hwai Tsai, Angeline Wu, et al. "Acquisition of NOTCH dependence is a hallmark of human intestinal stem cell maturation." Stem Cell Reports. 2022 May 10;17(5):1138-1153. PMID: 35395175
    2. Ireland AS, Micinski AM, et al. "MYC Drives Temporal Evolution of Small Cell Lung Cancer Subtypes by Reprogramming Neuroendocrine Fate." Cancer Cell. 2020;S1535-6108(20)30218-X. PMID: 32473656
    3. Zhu M, Li Y, et al. "Effects of bisphenol A and its alternative bisphenol F on Notch signaling and intestinal development: A novel signaling by which bisphenols disrupt vertebrate development." Environ Pollut. 2020;263(Pt B):114443. PMID: 32311622
    4. Zhu M, Niu Y, et al. "Low Concentrations of Tetrabromobisphenol A Disrupt Notch Signaling and Intestinal Development in in Vitro and in Vivo Models." Chem Res Toxicol. 2020;10.1021/acs.chemrestox.9b00528. PMID: 32041402
    5. Idowu J, Home T, et al. "Aberrant Regulation of Notch3 Signaling Pathway in Polycystic Kidney Disease." Sci Rep. 2018 Feb 20;8(1):3340. PMID: 29463793

YO-01027 (Dibenzazepine, DBZ)

Background

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