Overview

  • 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.
  • Purity

    > 99%
  • CAS Number

    209986-17-4
  • Chemical structure

    Chemical Structure

Properties

  • 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.

  • 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

  • Research areas

Applications

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
Functional Studies Use at an assay dependent concentration.

Images

  • 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.

References

This product has been referenced in:

  • Grimwood S  et al. Determination of guinea-pig cortical gamma-secretase activity ex vivo following the systemic administration of a gamma-secretase inhibitor. Neuropharmacology 48:1002-11 (2005). Read more (PubMed: 15857627) »
  • Campbell WA  et al. Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from gamma-secretase. J Neurochem 85:1563-74 (2003). Read more (PubMed: 12787075) »
  • Seiffert D  et al. Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors. J Biol Chem 275:34086-91 (2000). Read more (PubMed: 10915801) »
See all 2 Publications for this product

Customer reviews and Q&As

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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