Name: JLK 6
Price: 447.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    JLK 6, an isocoumarin, is a selective inhibitor of γ-secretase, with an IC50 value between 10 μM-1 mM [1, 2].The enzyme γ-secretase catalyzes the cleavage of β-Amyloid precursor protein (βAPP) to produce Amyloid β-peptide (Aβ). Aβ is a part of the plaque present in the brain of patients with Alzheimer’s disease. γ-secretase also targets other substrates like Notch. Notch is a transmembrane protein which is involved in important functions during different stages in development, both embryonic and adulthood [1].HEK293 cells were used. In these cells, wild-type βAPP was overexpressed (962 fmol/mL in 35-mm wells). JLK6 markedly reduced Aβ secreted from these cells. Interestingly, JLK6 potentiated the recovery of two fragments. Immunological characterization indicated that one fragment was labelled with a specific antibody against the Asp1 residue of Aβ. JLK6 also inhibited the Aβ recovery from cells overexpressing Swedish-mutant βAPP to a similar extent [2].In the zebrafish embryo, JLK isocoumarin inhibitors did not change the Notch pathway responsible for somitogenesis. Unlike other γ-secretase inhibitors, these agents did not affect E-cadherin processing. JLKs did not inhibit α-secretase, β-site APP cleaving enzymes (BACE) 1 and BACE2, GSK3β kinase and proteasome. JLK inhibitors prevented Aβ production without inducing unwanted cleavages of other proteins [1].
    
    [1]. Petit A, Pasini A, Alves Da Costa C, et al. JLK isocoumarin inhibitors: Selective γ-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo. Journal of neuroscience research, 2003, 74(3): 370-377.
    [2]. Petit A, Bihel F, da Costa CA, et al. New protease inhibitors prevent γ-secretase-mediated production of Aβ40/42 without affecting Notch cleavage. Nature cell biology, 2001, 3(5): 507-511.
- Properties
  - Alternative Name
    
    7-Amino-4-chloro-3-methoxy-1H-2-benzopyran; 7-amino-4-chloro-3-methoxy-1H-isochromen-1-one
    
    CAS Number
    
    62252-26-0
    
    Molecular Formula
    
    C10H8ClNO3
    
    Molecular Weight
    
    225.63
    
    Appearance
    
    Yellow solid
    
    Purity
    
    98.00%
    
    Solubility
    
    <22.56mg/ml in DMSO; <5.64mg/ml in ethanol
    
    Storage
    
    Store at RT
    
    * For Research Use Only

JLK 6

JLK 6

Background

We Also Recommend

Begacestat

L-685,458

MRK 560