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565790 Sigma-Aldrich

γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem

This g-secretase inhibitor, CAS 209986-17-4, is a cell-permeable, potent, selective, non-transition-state analog inhibitor of γ-secretase and Notch processing. Lowers Aβ levels in APP transgenic mice

Synonym: (S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, Compound E

  • CAS Number 209986-17-4

  • Linear Formula C₂₇H₂₄F₂N₄O₃

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Properties

Related Categories Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology More...
brand family   Calbiochem
packaging   1 mg in Glass bottle (565790-1MG)
  500 μg in Plastic ampoule (565790-500UG)
ATP competitive   N
form   White solid
reversible   N
primary target   γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
primary target IC50   300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40
purity   ≥95% by HPLC
cell permeable   Y
toxicity   Standard Handling
shipped in   ambient
storage temp.   +2C to +8C
storage conditions   Protect from light
  Ok to freeze

Description

Overview

A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC50 = 300 pM for Aβ40 in CHO cells overexpressing wild type βAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40 and Aβ42 in SH-SY5Y cells stably transfected with SPA4CT). Lowers Aβ levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM).

Packaging

Packaged under inert gas

Storage and Shipping Instructions

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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