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YO-01027 (Dibenzazepine, DBZ)γ-secretase inhibitor

YO-01027 (Dibenzazepine, DBZ)

Catalog No. A4018
Size Price Stock Qty
10mM (in 1mL DMSO) $210.00 In stock
Evaluation Sample $28.00 In stock
5mg $130.00 In stock
10mg $240.00 In stock
25mg $470.00 In stock
50mg $590.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

YO-01027 (Dibenzazepine, DBZ)

Related Biological Data

YO-01027 (Dibenzazepine, DBZ)

Related Biological Data

YO-01027 (Dibenzazepine, DBZ)

Related Biological Data

YO-01027 (Dibenzazepine, DBZ)

Biological Activity

Description YO-01027 (Dibenzazepine, DBZ) is a dipeptidic inhibitor of γ-secretase with IC50 of 2.6 nM and 2.9 nM for APPL and Notch cleavage, respectively.
Targets APPL Notch        
IC50 2.6 nM 2.9 nM        

YO-01027 (Dibenzazepine, DBZ) Dilution Calculator

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Chemical Properties

Cas No. 209984-56-5 SDF Download SDF
Synonyms gamma-Secretase Inhibitor XX,YO01027
Chemical Name (2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide
Canonical SMILES CC(C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)CC4=CC(=CC(=C4)F)F
Formula C26H23F2N3O3 M.Wt 463.48
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

YO-01027, also known as dibenzazepine or DBZ, is a potent inhibitor of γ-secretase, a multisubunit aspartyl protease catalyzing the cleavage of numerous type I integral membrane proteins (such as amyloid precursor protein (APP) and Notch). YO-01027 also potently blocks amyloid precursor protein-like (APPL) and Notch cleavage, with estimated inhibition constant IC50 of 2.640.30 nM and 2.920.22 nM respectively, through interaction with the N-terminal fragment of Presenilin in a dose-response manner. Recent studies show that YO-01027-induced inhibition Notch signaling pathway leads to a rapid conversion of proliferative crypt cells into postmitotic cells and impairs MUC16 biosynthesis in a concentration-dependent manner in undifferentiated cells instead of postmiotic stratified cells at both preconfluent and confluent stages.

Reference

Linjie Xiong, Ashley M. Woodward, and Pablo Argueso. Notch signaling modulates MUC16 biosynthesis in an vitro model of human corneal and conjunctival epithelial cell differentiation. Invest. Ophthalmol. Vis. Sci. 2011, 52(8), 5641-5646

Casper Groth, W. Gregory Alvord, Octavio A. Quinones, and Mark E. Fortini. Pharmacological analysis of drosphila melanogaster γ-secretase with respect to differential proteolysis of Notch and APP. Mol. Pharmacol. 2010, 77(4), 567-574