DBZ

Tocris Bioscience a Bio-Techne Brand

Catalog # 4489

Citations (11)

(1)

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Key Product Details

Description:	γ-secretase inhibitor; inhibits Notch pathway
Alternative Names:	Dibenzazepine, YO-01027
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% (HPLC)
Molecular Weight:	463.48

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Biological Activity for DBZ

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 naïve-state pluripotency in non-hypoxic conditions.

DBZ synthesized to Ancillary Material Grade also available.

Compound Libraries for DBZ

DBZ is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for DBZ

M. Wt	463.48
Formula	C₂₆H₂₃F₂N₃O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	209984-56-5
PubChem ID	11454028
InChi Key	QSHGISMANBKLQL-OWJWWREXSA-N
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

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.

Solubility for DBZ

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	46.35	100

Preparing Stock Solutions for DBZ

The following data is based on the product molecular weight 463.48.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.16 mL	10.79 mL	21.58 mL
5 mM	0.43 mL	2.16 mL	4.32 mL
10 mM	0.22 mL	1.08 mL	2.16 mL
50 mM	0.04 mL	0.22 mL	0.43 mL

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References for DBZ

References are publications that support the biological activity of the product.

Wu Dibenzazepine promotes cochlear supporting cell proliferation and hair cell regeneration in neonatal mice. Cell Prolif. 2020 PMID: 32677724
Isono The combination of dibenzazepine and a DOT1L inhibitor enables a stable maintenance of human naïve-state pluripotency in non-hypoxic conditions. Regen.Ther. 2020 PMID: 33426214
Ichida Notch inhibition allows oncogene-independent generation of iPS cells. Nat.Chem.Biol. 2014 PMID: 24952596
Groth Pharmacological analysis of Drosophila melanogaster γ-secretase with respect to differential proteolysis of Notch and APP. Mol.Pharmacol. 2010 PMID: 20064975
van Es Notch/γ-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cells. Nature 2005 PMID: 15959515

Citations for DBZ (11)

Showing 1 - 10 of 11 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for DBZ include:

Page et al. (2019) Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis. Cell Rep. 27:3139
PMID: 31189101
Yung et al. (2019) Sufu- And Spop-mediated downregulation of Hedgehog signaling promotes beta cell differentiation through organ-specific niche signals. Nat.Commun.. 10:4647
PMID: 31604927
Santos et al. (2019) Urothelial organoids originating from Cd49f^high mouse stem cells display Notch-dependent differentiation capacity. Nat.Commun.. 10:4407
PMID: 31562298
Khan et al. (2018) The deubiquitinase USP9X regulates FBW7 stability and suppresses colorectal cancer. J Clin Invest. 128:1326
PMID: 29346117
Chen et al. (2018) Cancer-associated fibroblasts suppress SOX2-induced dysplasia in a lung squamous cancer coculture. Proc Natl Acad Sci U S A. 115:E11671
PMID: 30487219
Marshall et al. (2018) Analysis of the Intrinsic Self-Organising Properties of Mesenchymal Stromal Cells in Three-Dimensional Co-Culture Models with Endothelial Cells. Bioengineering (Basel). 5
PMID: 30373192
Bi et al. (2016) Stage-specific effects of Notch activation during skeletal myogenesis. Elife. 5
PMID: 27644105
Ihara et al. (2016) TGF-β Signaling in Dendritic Cells Governs Colonic Homeostasis by Controlling Epithelial Differentiation and the Luminal Microbiota. J Immunol. 196:4603
PMID: 27183608
Bi et al. (2016) Notch activation drives adipocyte dedifferentiation and tumorigenic transformation in mice. J Exp Med. 213:2019
PMID: 27573812
Bi et al. (2014) Inhibition of Notch signaling promotes browning of white adipose tissue and ameliorates obesity. Nat Med. 20:911
PMID: 25038826
Shah et al. (2013) The role of Notch and γ-secretase inhibition in an ovarian cancer model. J Reprod Dev. 33:801
PMID: 23482747

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Customer Reviews for DBZ (1)

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DBZ

Name: Minjin Jeong

Species: Mouse

Assay Type: In Vivo

Cell Line/Tissue: iPSCs

Differentiation of hiPSCs into optic progenitor cells.

For obtaining a higher solubility, I recommend warming at 37°C.

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Product Documents for DBZ

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.

DBZ