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DBZ

Catalog #: 4489
21 Citations Datasheet
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DBZ | CAS No. 209984-56-5 | Secretase Inhibitors
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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%

Product Details
Citations (21)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
463.48
Formula:
C26H23F2N3O3
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
209984-56-5

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

  1. Glycoprotein 2 is a specific cell surface marker of human pancreatic progenitors
    KF Cogger, A Sinha, F Sarangi, EC McGaugh, D Saunders, C Dorrell, S Mejia-Guer, Y Aghazadeh, JL Rourke, RA Screaton, M Grompe, PR Streeter, AC Powers, M Brissova, T Kislinger, MC Nostro
    Nat Commun, 2017;8(1):331.
  2. Cancer-associated fibroblasts suppress SOX2-induced dysplasia in a lung squamous cancer coculture
    S Chen, A Giannakou, S Wyman, J Gruzas, J Golas, W Zhong, C Loreth, L Sridharan, TT Yamin, M Damelin, KG Geles
    Proc. Natl. Acad. Sci. U.S.A., 2018;115(50):E11671-E11680.
  3. Transcription factor PROX1 suppresses Notch pathway activation via the nucleosome remodeling and deacetylase complex in colorectal cancer stem-like cells
    J Högström, S Heino, P Kallio, M Lähde, VM Leppänen, D Balboa, Z Wiener, K Alitalo
    Cancer Res., 2018;0(0):.
  4. Notch inhibition allows oncogene-independent generation of iPS cells.
    Ichida et al.
    Nat.Chem.Biol., 2014;10:632
  5. Pharmacological analysis of Drosophila melanogaster γ-secretase with respect to differential proteolysis of Notch and APP.
    Groth et al.
    Mol.Pharmacol., 2010;77:567
  6. 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:

21 Citations: Showing 1 - 10

  1. Contribution of Trp63CreERT2-labeled cells to alveolar regeneration is independent of tuft cells.
    Authors: Timothy C Et al.
    Elife  2022;11
  2. Mapping the temporal and spatial dynamics of the human endometrium in vivo and in vitro.
    Authors: Cecilia Et al.
    Nat Genet  2021;53:1698-1711
  3. Principles of signaling pathway modulation for enhancing human naive pluripotency induction.
    Authors: Varda Et al.
    Cell Stem Cell  2021;28:1549-1565.e12
  4. Commitment and oncogene-induced plasticity of human stem cell-derived pancreatic acinar and ductal organoids.
    Authors: Ling Et al.
    Cell Stem Cell  2021;28:1090-1104.e6
  5. Direct SARS-CoV-2 infection of the human inner ear may underlie COVID-19-associated audiovestibular dysfunction.
    Authors: Karen E Et al.
    Commun Med (Lond)  2021;1:44
  6. Soluble guanylate cyclase signalling mediates etoposide resistance in progressing small cell lung cancer.
    Authors: Cong Et al.
    Nat Commun  2021;12:6652
  7. The Transcription Co-Repressors MTG8 and MTG16 Regulate Exit of Intestinal Stem Cells From Their Niche and Differentiation Into Enterocyte vs Secretory Lineages.
    Authors: Harshil Et al.
    Gastroenterology  2020;159:1328-1341.e3
  8. A Notch3-Marked Subpopulation of Vascular Smooth Muscle Cells Is the Cell of Origin for Occlusive Pulmonary Vascular Lesions.
    Authors: Fan Et al.
    Circulation  2020;142:1545-1561
  9. Resolving the fibrotic niche of human liver cirrhosis at single-cell level.
    Authors: S A Et al.
    Nature  2019;575:512-518
  10. Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis.
    Authors: Page Et al.
    Cell Rep  2019;27:3139
  11. 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
  12. Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity.
    Authors: Santos Et al.
    Nat.Commun.  2019;10:4407
  13. Transcription Factor PROX1 Suppresses Notch Pathway Activation via the Nucleosome Remodeling and Deacetylase Complex in Colorectal Cancer Stem-like Cells.
    Authors: Kari Et al.
    Cancer Res  2018;78:5820-5832
  14. 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
  15. The deubiquitinase USP9X regulates FBW7 stability and suppresses colorectal cancer.
    Authors: Khan Et al.
    J Clin Invest  2018;128:1326
  16. 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
  17. Stage-specific effects of Notch activation during skeletal myogenesis.
    Authors: Bi Et al.
    Elife  2016;5
  18. Notch activation drives adipocyte dedifferentiation and tumorigenic transformation in mice.
    Authors: Bi Et al.
    J Exp Med  2016;213:2019
  19. 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
  20. Inhibition of Notch signaling promotes browning of white adipose tissue and ameliorates obesity.
    Authors: Bi Et al.
    Nat Med  2014;20:911
  21. 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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