CAS NO: | 62252-26-0 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Cas No. | 62252-26-0 |
别名 | 7-Amino-4-chloro-3-methoxy-1H-2-benzopyran |
化学名 | 7-amino-4-chloro-3-methoxy-1H-isochromen-1-one |
Canonical SMILES | COC1=C(Cl)C2=CC=C(N)C=C2C(O1)=O |
分子式 | C10H8ClNO3 |
分子量 | 225.63 |
溶解度 | <22.56mg/ml in DMSO;<5.64mg/ml in ethanol |
储存条件 | Store at RT |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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]. References: |