YO-01027
Based on 8 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.59%
- No. CAS: 209984-56-5
- Fòrmula: C26H23F2N3O3
- Peso molecular:463.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) YO-01027
More- Science. 2024 Dec 13;386(6727):eado5561. [Abstract]
- Nat Genet. 2023 Apr;55(4):651-664. [Abstract]
- Cell Commun Signal. 2025 Oct 1;23(1):403. [Abstract]
- EMBO J. 2024 Sep;43(18):3916-3947. [Abstract]
- Med Oncol. 2021 Mar 17;38(4):41. [Abstract]
- iScience. 2026 May 25;29(6):116079. [Abstract]
- FASEB J. 2023 Feb;37(2):e22743. [Abstract]
- bioRxiv. 2026 Jan 17.
Customer Validation & Images
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Others
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WB
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Cell Imaging/Staining
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Actividad biológica
IC50: 2.92±0.22 (Notch), 2.64±0.30 (APPL) nM[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 209984-56-5
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Appearance Solid
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Peso molecular 463.48
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Fòrmula C26H23F2N3O3
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Color White to off-white
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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
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Synonyms
Dibenzazepine; DBZ
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Science
An injury-induced mesenchymal-epithelial cell niche coordinates regenerative responses in the lung. [Abstract]2024 Dec 13;386(6727):eado5561. PMID: 39666855 -
Nat Genet
2023 Apr;55(4):651-664. PMID: 36914834 -
Cell Commun Signal
The aggressive colorectal cancer subtype marker HTR2B has a dual role depending on the tumor microenvironment. [Abstract]2025 Oct 1;23(1):403. PMID: 41034989
YO-01027 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Oct 1;23(1):403. [Abstract]
The effect of the NOTCH inhibitor DAPT and DBZ (10 µM) on the organoid and invasion area in collagen-I.
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EMBO J
2024 Sep;43(18):3916-3947. PMID: 39085648
YO-01027 purchased from MedChemExpress. Usage Cited in: EMBO J. 2024 Sep;43(18):3916-3947. [Abstract]
Expression levels of Dclk1, ChgA, and β-actin in the small intestine of Elp3 WT and Elp3 ΔIEC mice (untreated or treated with dibenzodiazepines (DBZ: 15 μmol/kg)) were detected by Western blot.
YO-01027 purchased from MedChemExpress. Usage Cited in: EMBO J. 2024 Sep;43(18):3916-3947. [Abstract]
Immunostaining of clustered cells (Dclk1+ cells, red) in the small intestine of Elp3 WT and Elp3 ΔIEC mice (treated with or untreated with DBZ (15 μmol/kg)).
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Med Oncol
Targeting Hedgehog signalling in CD133-positive hepatocellular carcinoma: improving Lenvatinib therapeutic efficiency. [Abstract]2021 Mar 17;38(4):41. PMID: 33730237 -
iScience
Ciclopirox reprograms effector responses and modulates Notch1 activation in activated human T cells. [Abstract]2026 May 25;29(6):116079. PMID: 42239721 -
FASEB J
Deficiency of thrombospondin-2 alleviates intimal hyperplasia in mice by modulating vascular smooth muscle cell proliferation and migration. [Abstract]2023 Feb;37(2):e22743. PMID: 36645109 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Groth C, et al. Pharmacological analysis of Drosophila melanogaster gamma-secretase with respect to differential proteolysis of Notch and APP. Mol Pharmacol. 2010 Apr;77(4):567-74. [Content Brief]
[2]. Fuwa H, et al. Divergent synthesis of multifunctional molecular probes to elucidate the enzyme specificity of dipeptidic gamma-secretase inhibitors. ACS Chem Biol. 2007 Jun 15;2(6):408-18. [Content Brief]
[3]. Zheng YH, et al. Notch γ-secretase inhibitor dibenzazepine attenuates angiotensin II-induced abdominal aortic aneurysm in ApoE knockout mice by multiple mechanisms. PLoS One. 2013 Dec 16;8(12):e83310. [Content Brief]
[4]. Xiao Z, et al. The Notch γ-secretase inhibitor ameliorates kidney fibrosis via inhibition of TGF-β/Smad2/3 signaling pathway activation. Int J Biochem Cell Biol. 2014 Oct;55:65-71. [Content Brief]
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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