RGNCY-0018 (Tau phosphorylation & B-amyloid aggregation Inhibitor)
The most important pathogenic brain changes contributing to the development of Alzheimer’s disease are the formation of the cytotoxic β -amyloid aggregates and of the neurofibrillary tangles, which originate from amyloid-β peptides and hyperphosphorylated tau protein, respectively. Compound 8 represents a novel bis(hydroxyphenyl)-substituted thiophene that is a selective, dual inhibitors of the tau kinase Dyrk1A (IC50 = 0.5uM) and of the amyloid-β aggregation (91+1% inhibition at 100uM).
Systematic Name: 4,4'-(thiophene-2,5-diyl)bis(2-methylphenol)
Molecular Weight: 296.38
Reference: Mariano, Marica, et. al. "First Selective Dual Inhibitors of Tau Phosphorylation and Beta-Amyloid Aggregation, Two Major Pathogenic Mechanisms in Alzheimer’s Disease" ACS Chemical Neuroscience (2014)
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Tags: Kinase, Alzheimer’s, Amyloid, Tau, Dyrk1A, Alzheimers, Alzheimer, RGNCY-0018, Phosphorylation, B-amyloid