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

YO-01027 (Synonyms: Dibenzazepine; DBZ)

Cat. No.: HY-13526 Purity: 98.03%
Handling Instructions

YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 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
Solution
10 mM * 1 mL in DMSO USD 108 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 108 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 106 In-stock
Estimated Time of Arrival: December 31
10 mg USD 185 In-stock
Estimated Time of Arrival: December 31
25 mg USD 422 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE YO-01027

    YO-01027 purchased from MCE. Usage Cited in: J Clin Invest. 2020 Feb 3;130(2):612-624.

    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. 2020 Feb 3;130(2):612-624.

    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

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    • References

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    Description

    YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 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].

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

    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].

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

    Molecular Weight

    463.48

    Formula

    C26H23F2N3O3

    CAS No.
    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 (ultrasonic;warming;heat to 60°C) (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 available 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: 98.67%

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    Product Name:
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    Cat. No.:
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