YO-01027 Inhibitor CAS No. 209984-56-5

Cat. No.	Name	Size	Price
KI0490	YO-01027	2 mg	$232
	YO-01027	5 mg	$330
	YO-01027	25 mg	$1100
	YO-01027	100 mg	$3600

Chemical Characteristic

Product Name	YO-01027
Synonyms	Dibenzazepine, DBZ
CAS No.	209984-56-5
Molecular Weight	463.48
Formula	C₂₆H₂₃F₂N₃O₃
Chemical Name	(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide
Smiles	C(=O)([C@H](C)NC(=O)Cc1cc(cc(c1)F)F)NC1C(=O)N(c2c(c3c1cccc3)cccc2)C
Chemical Structure

Biological activities

YO-01027 is a potent γ-secretase inhibitor. The IC50 of YO-01027 is 2.6 and 2.9 nM against Notch and APPL cleavage sensitivities, respectively. YO-01027 blocks Notch signaling. YO-01027 interacts directly with the γ-secretase complex and targets different functional domains of the complex. YO-01027 targets the N-terminal Presenilin fragment. ^[1] YO-01027 stops Notch-ICD cleavage and its subsequent nuclear translocation. YO-01027 significantly decreases MCF7 but not MDA-MB-231 tumours.^[2] In DDC treated wild type mice, pharmacologic Notch inhibition with YO-01027 decreases the number of both ductular reaction and hepatic progenitor cells. ^[3]

Protocols

YO-01027 is dissolved in 0.5% Methocel, 0.1% Tween80.^[2]

References

[1] Xiong L, et al. Notch signaling modulates MUC16 biosynthesis in an in vitro model of human corneal and conjunctival epithelial cell differentiation. Invest Ophthalmol Vis Sci. 2011, 52(8): 5641-5646. [2] Harrison H, et al. Regulation of breast cancer stem cell activity by signaling through the Notch4 receptor. Cancer Res. 2010, 70(2): 709-718. [3] Fiorotto R, et al. Notch signaling regulates tubular morphogenesis during repair from biliary damage in mice. J Hepatol. 2013.

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