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DBZ [Notch; APPL Inhibitor]

[CAT#: MOD2005ZP79]

γ-secretase and Notch pathway inhibitor. Stimulates iPSC formation.

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Synonyms
Dibenzazepine; YO-01027
Chemical Name
N-[(1S)-2-[[(7S)-6,7-Dihydro-5-meth yl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl -2-oxoethyl]-3,5-difluorobenzeneacetamide
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
Increasing the concentration of DBZ in cells expressing APPL or Notch will lead to the gradual accumulation of APPL CTF fragments and reduce the production of NICD in a strict dose-dependent manner [1]. The molecular targets of CE and DBZ are the N-terminal fragments of presenilin 1 in the γ-secretase complex [2].
Reference
[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.
Assay Description
DBZ blocked activated Notch1 signaling in Apo E-/- mice injected with Ang II and human abdominal aortic aneurysm (AAA) tissue undergoing AAA repair. DBZ significantly prevented the accumulation of macrophages and CD4 + T cells stimulated by Ang II, and ERK-mediated angiogenesis simultaneously reversed the Th2 response in vivo [1]. The use of DBZ significantly reduced the expression of renal fibrosis and fibrosis markers, including collagen 1α1/3α1, fibronectin and α-smooth muscle actin. DBZ significantly inhibits the expression of transforming growth factor (TGF)-β, phosphorylated Smad 2 and Smad 3 induced by ureteral occlusion [2].
References
[1]. 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.

[2]. 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.
Molecular Weight
463.48
Form
Powder
Chemical Formula
C26H23F2N3O3
Source
Synthetic
SMILES
CN1C2=C(C=CC=C2)C3=C(C=CC=C3)[C@H](NC([C@@H](NC(CC4=CC(F)=CC(F)=C4)=O)C)=O)C1=O
Solubility
Soluble in DMSO (100mM)
IC50
2.92±0.22nM (Notch); 2.64±0.30nM (APPL)
CAS NO.
209984-56-5
PubChem Substance ID
11454028
Purity
>98%
Storage
-20°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -33°C for several months.
Research Use Only
For research use only

For Research Use Only. Not For Clinical Use.
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