DBZ
Chemical Name: N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluorobenzeneacetamide
Purity: ≥98%
Biological Activity
DBZ is an inhibitor of γ-secretase aspartyl protease. DBZ blocks amyloid precursor protein-like (APPL) and Notch cleavage (IC50 values are 2.6 nM and 1.7-2.9 nM, respectively). By inhibiting Notch and the Notch pathway, DBZ improves efficiency of iPSC generation and production of iPSCs from mouse and human keratinocytes without KLF4 and CMYC. In an animal model of Alzheimer's disease, DBZ inhibits the cleavage of amyloid precursor protein into Aβ40. DBZ promotes cochlear supporting cell proliferation and hair cell mitotic regeneration in neonatal mice. DBZ in combination with iDOT1L enables maintenance of human na�ve-state pluripotency in non-hypoxic conditions.DBZ synthesized to Ancillary Material Grade also available.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Notch inhibition allows oncogene-independent generation of iPS cells.
Ichida et al.
Nat.Chem.Biol., 2014;10:632 -
Pharmacological analysis of Drosophila melanogaster γ-secretase with respect to differential proteolysis of Notch and APP.
Groth et al.
Mol.Pharmacol., 2010;77:567 -
Notch/γ-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cells.
van Es et al.
Nature, 2005;435:959
Product Datasheets
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Citations for DBZ
The citations listed below are publications that use Tocris products. Selected citations for DBZ include:
11 Citations: Showing 1 - 10
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Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis.
Authors: Page Et al.
Cell Rep 2019;27:3139
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Sufu- And Spop-mediated downregulation of Hedgehog signaling promotes beta cell differentiation through organ-specific niche signals.
Authors: Yung Et al.
Nat.Commun. 2019;10:4647
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Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity.
Authors: Santos Et al.
Nat.Commun. 2019;10:4407
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Analysis of the Intrinsic Self-Organising Properties of Mesenchymal Stromal Cells in Three-Dimensional Co-Culture Models with Endothelial Cells.
Authors: Marshall Et al.
Bioengineering (Basel) 2018;5
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The deubiquitinase USP9X regulates FBW7 stability and suppresses colorectal cancer.
Authors: Khan Et al.
J Clin Invest 2018;128:1326
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Cancer-associated fibroblasts suppress SOX2-induced dysplasia in a lung squamous cancer coculture.
Authors: Chen Et al.
Proc Natl Acad Sci U S A 2018;115:E11671
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Stage-specific effects of Notch activation during skeletal myogenesis.
Authors: Bi Et al.
Elife 2016;5
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Notch activation drives adipocyte dedifferentiation and tumorigenic transformation in mice.
Authors: Bi Et al.
J Exp Med 2016;213:2019
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TGF-β Signaling in Dendritic Cells Governs Colonic Homeostasis by Controlling Epithelial Differentiation and the Luminal Microbiota.
Authors: Ihara Et al.
J Immunol 2016;196:4603
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Inhibition of Notch signaling promotes browning of white adipose tissue and ameliorates obesity.
Authors: Bi Et al.
Nat Med 2014;20:911
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The role of Notch and γ-secretase inhibition in an ovarian cancer model.
Authors: Shah Et al.
J Reprod Dev 2013;33:801
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