1. Neuronal Signaling
    Stem Cell/Wnt
  2. Notch
    γ-secretase
  3. YO-01027

YO-01027 (Synonyms: Dibenzazepine; DBZ)

Cat. No.: HY-13526 Purity: 99.23% ee.: 99.36%
Handling Instructions

YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92±0.22 and 2.64±0.30 nM for Notch and APPL cleavage, respectively.

For research use only. We do not sell to patients.

YO-01027 Chemical Structure

YO-01027 Chemical Structure

CAS No. : 209984-56-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 98 In-stock
Estimated Time of Arrival: December 31
2 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
25 mg USD 384 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE YO-01027

    YO-01027 purchased from MCE. Usage Cited in: J Clin Invest. 2019 Oct 31. pii: 126896. 

    Immunoblotting of the indicated proteins in PC9GR cells treated with vehicle (DMSO), DBZ (250 nM) or gefitinib (1 μM). This is a representative image of three different experiments.

    YO-01027 purchased from MCE. Usage Cited in: J Clin Invest. 2019 Oct 31. pii: 126896. 

    Immunoblotting of the indicated proteins in CHO cells transfected with pBabe empty vector or pEGFRT790M/L858R and treated with vehicle (DMSO) or DBZ (250 nM) and/or gefitinib (1 μM). This is a representative image of two different experiments.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92±0.22 and 2.64±0.30 nM for Notch and APPL cleavage, respectively.

    IC50 & Target

    IC50: 2.92±0.22 (Notch), 2.64±0.30 (APPL) nM[1]

    In Vitro

    Increasing concentrations of DBZ 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]. The molecular targets of CE and DBZ are the N-terminal fragment of presenilin 1 within the γ-secretase complex[2].

    In Vivo

    DBZ blocks activated Notch1 signaling in abdominal aortic aneurysm (AAA) tissue from both Ang II-infused Apo E-/- mice and human undergoing AAA repair. DBZ markedly prevents Ang II-stimulated accumulation of macrophages and CD4+ T cells, and ERK-mediated angiogenesis, simultaneously reverses Th2 response, in vivo[3]. Administration of DBZ markedly attenuates renal fibrosis and expression of fibrotic markers, including collagen 1α1/3α1, fibronectin, and α-smoothmuscle actin. DBZ significantly inhibits ureteral obstruction -induced expression of transforming growth factor (TGF)- β, phosphorylated Smad 2, and Smad 3[4].

    Molecular Weight

    463.48

    Formula

    C₂₆H₂₃F₂N₃O₃

    CAS No.

    209984-56-5

    SMILES

    O=C(N[[email protected]@H](C)C(N[[email protected]]1C2=CC=CC=C2C3=CC=CC=C3N(C)C1=O)=O)CC4=CC(F)=CC(F)=C4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (71.20 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1576 mL 10.7880 mL 21.5759 mL
    5 mM 0.4315 mL 2.1576 mL 4.3152 mL
    10 mM 0.2158 mL 1.0788 mL 2.1576 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (5.39 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.39 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    DBZ (0.1, 1, 2.5, 5, 7.5, 10, 25, 50, 100, 250 nM) are added to the S2 cell medium upon induction of Notch or APPL expression, 6 h before protein harvesting. For each sample, the same inhibitor is also included at the corresponding concentration in the lysis buffer for protein extraction and immunoblot analysis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice: Male wild-type (WT) C57BL/6J and Apo E-/- mice are used in the study. Ang II-treated mice are received an intraperitoneal injection of either saline vehicle or γ-secretase inhibitor, dibenzazepine (DBZ) (1 mg/kg/d, dissolved in saline) 1 day before mini-pump implantation, and the treatment continued daily for 4 weeks. The blood pressure is measured in conscious mice using a computerized tail-cuff system. All mice are anesthetized. The aortic tissues are removed and prepared for further histological and molecular analysis[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.23% ee.: 99.36%

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    Cat. No.:
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