Compound E, gamma;-secretase inhibitor (ab142164)
Key features and details
- Cell-permeable, selective, non-competitive, potent γ-secretase inhibitor
- CAS Number: 209986-17-4
- Purity: > 99%
- Soluble in DMSO to 100 mM
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
Compound E, gamma;-secretase inhibitor -
Description
Cell-permeable, selective, non-competitive, potent γ-secretase inhibitor -
Biological description
Cell-permeable, selective, non-competitive, potent γ-secretase inhibitor (IC50 = 0.3 nM). Active in vitro and in vivo.
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Purity
> 99% -
CAS Number
209986-17-4 -
Chemical structure
Properties
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Chemical name
N-[(1S)-2-[[(3S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluorobenzeneacetamide -
Molecular weight
490.51 -
Molecular formula
C27H24F2N4O3 -
PubChem identifier
11306390 -
Storage instructions
Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
Solubility overview
Soluble in DMSO to 100 mM -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
C[C@@H](C(=O)N[C@@H]1C(=O)N(C2=CC=CC=C2C(=N1)C3=CC=CC=C3)C)NC(=O)CC4=CC(=CC(=C4)F)F -
Source
Synthetic
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Research areas
Applications
The Abpromise guarantee
Our Abpromise guarantee covers the use of ab142164 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
Application | Abreviews | Notes |
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Functional Studies |
Use at an assay dependent concentration.
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Notes |
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Functional Studies
Use at an assay dependent concentration. |
Images
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2D chemical structure image of ab142164, Compound E, gamma;-secretase inhibitor
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Kc167 cells were treated with varying concentrations of compound E (ab142164) in DMSO for 16hr at 25°C; DMSO only was used as the negative control. The cells were further incubated for 30 minutes with 4mM EGTA in PBS (in the presence of compound E), and were then lysed for analysis. To measure Notch activity, Notch targets E(spl)mβ-HLH and E(spl)m3-HLH mRNA levels were assayed. Data shows the fold change of mRNA levels of E(spl)mβ-HLH and E(spl)m3-HLH under different conditions, normalised to DMSO treatment (negative control). Notch activation by EGTA is abrogated by treatment with compound E.
Protocols
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
References (7)
ab142164 has been referenced in 7 publications.
- Alhashem Z et al. Notch controls the cell cycle to define leader versus follower identities during collective cell migration. Elife 11:N/A (2022). PubMed: 35438077
- Zhang YF et al. MicroRNA-582-5p Contributes to the Maintenance of Neural Stem Cells Through Inhibiting Secretory Protein FAM19A1. Front Cell Neurosci 16:866020 (2022). PubMed: 35685988
- Taga A et al. Establishment of an Electrophysiological Platform for Modeling ALS with Regionally-Specific Human Pluripotent Stem Cell-Derived Astrocytes and Neurons. J Vis Exp N/A:N/A (2021). PubMed: 34515684
- Naylor RW et al. A novel mechanism of gland formation in zebrafish involving transdifferentiation of renal epithelial cells and live cell extrusion. Elife 7:N/A (2018). PubMed: 30394875
- Kang Y et al. Improving Cell Survival in Injected Embryos Allows Primed Pluripotent Stem Cells to Generate Chimeric Cynomolgus Monkeys. Cell Rep 25:2563-2576.e9 (2018). PubMed: 30485820
- Liu X et al. BMP9 overexpressing adipose-derived mesenchymal stem cells promote cartilage repair in osteoarthritis-affected knee joint via the Notch1/Jagged1 signaling pathway. Exp Ther Med 16:4623-4631 (2018). PubMed: 30542413
- Slaninova V et al. Notch stimulates growth by direct regulation of genes involved in the control of glycolysis and the tricarboxylic acid cycle. Open Biol 6:150155 (2016). PubMed: 26887408