1. Stem Cell/Wnt
    Neuronal Signaling
  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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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].

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)

*"≥" 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.
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
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

Purity: 99.23% ee.: 99.36%

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Product Name:
YO-01027
Cat. No.:
HY-13526
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YO-01027

Cat. No.: HY-13526