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

YO-01027  (Synonyms: Dibenzazepine; DBZ)

Cat. No.: HY-13526 Purity: 99.94% ee.: 100.00%
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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

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of YO-01027:

YO-01027 Related Antibodies

Top Publications Citing Use of Products

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

    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.

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

    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.

    • 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 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].

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

    YO-01027 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    463.48

    Formula

    C26H23F2N3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N[C@@H](C)C(N[C@H]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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 71.43 mg/mL (154.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    C2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94% ee.: 100.00%

    COA (253 KB) HNMR (207 KB) CNMR (137 KB) RP-HPLC (208 KB) NP-HPLC (497 KB) LCMS (87 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1576 mL 10.7880 mL 21.5759 mL 53.9398 mL
    5 mM 0.4315 mL 2.1576 mL 4.3152 mL 10.7880 mL
    10 mM 0.2158 mL 1.0788 mL 2.1576 mL 5.3940 mL
    15 mM 0.1438 mL 0.7192 mL 1.4384 mL 3.5960 mL
    20 mM 0.1079 mL 0.5394 mL 1.0788 mL 2.6970 mL
    25 mM 0.0863 mL 0.4315 mL 0.8630 mL 2.1576 mL
    30 mM 0.0719 mL 0.3596 mL 0.7192 mL 1.7980 mL
    40 mM 0.0539 mL 0.2697 mL 0.5394 mL 1.3485 mL
    50 mM 0.0432 mL 0.2158 mL 0.4315 mL 1.0788 mL
    60 mM 0.0360 mL 0.1798 mL 0.3596 mL 0.8990 mL
    80 mM 0.0270 mL 0.1348 mL 0.2697 mL 0.6742 mL
    100 mM 0.0216 mL 0.1079 mL 0.2158 mL 0.5394 mL
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    YO-01027 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    YO-01027209984-56-5Dibenzazepine DBZYO01027YO 01027Notchγ-secretaseGamma secretaseInhibitorinhibitorinhibit

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