YO-01027

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.

Product Specifications

CAS Number

[209984-56-5]

Product Name Alternative

Dibenzazepine; DBZ

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Notch; γ-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/YO-01027.html

Purity

99.59

Solubility

DMSO : 71.43 mg/mL (ultrasonic)

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

Molecular Formula

C26H23F2N3O3

Molecular Weight

463.48

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.|[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.