An inhibitor of BACE1 and PI3K (IC50s = 11.43 and 15.99 μM

LX2343 – 5 mg

Brand:
Cayman
CAS:
333745-53-2
Storage:
-20
UN-No:
Non-Hazardous - /

LX2343 is an inhibitor of β-site amyloid protein cleaving enzyme 1 (BACE1/β-secretase; IC50 = 11.43 μM) and PI3K (IC50 = 15.99 μM).{47505} It inhibits accumulation of Aβ (1-40) (Aβ40) and Aβ42 induced by streptozotocin (STZ; Item No. 13104) in both HEK293-APPSW and CHO-APP cells, which express mutant and wild-type amyloid precursor protein (APP), respectively, in a concentration-dependent manner. It also inhibits STZ-induced increases in JNK and APPThr668 phosphorylation as well as soluble APPβ (sAPPβ) protein levels. LX2343 (10 mg/kg per day) reduces levels of Aβ40 and Aβ42, as well as thioflavine S staining, in the cortex and hippocampus in the APP/PS1 transgenic mouse model of Alzheimer’s disease. It also reduces cortical levels of PI3K, Akt, and mTOR phosphorylation and accumulation of the autophagy substrate p62, indicating increased autophagy. LX2343 (10 mg/kg per day) decreases path length and escape latency time in the Morris water maze in APP/PS1 mice.  

 

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SKU: 27799 - 5 mg Category:

Description

An inhibitor of BACE1 and PI3K (IC50s = 11.43 and 15.99 μM, respectively); inhibits STZ-induced accumulation of Aβ40 and Aβ42 in both HEK293-APPSW and CHO-APP cells in a concentration-dependent manner; inhibits STZ-induced increases in JNK and APPThr668 phosphorylation as well as sAPPβ protein levels; reduces levels of Aβ40 and Aβ42, as well as thioflavine S staining, in cortex and hippocampus in the APP/PS1 transgenic mouse model of Alzheimer’s disease at 10 mg/kg/day; reduces cortical levels of p62 protein and PI3K, Akt, and mTOR phosphorylation; decreases path length and escape latency time in the Morris water maze in APP/PS1 mice at 10 mg/kg/day

Formal name: N-1,3-benzodioxol-5-yl-2-[(5-chloro-2-methoxyphenyl)(phenylsulfonyl)amino]-acetamide

Synonyms: 

Molecular weight: 474.9

CAS: 333745-53-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Cell Biology|Proteolysis|Lysosomal Proteases||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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