K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with an EC50 of 80 nM. IC50 value: 80 nM (EC50)Target: Amyloid-βin vitro: The active drug candidate K162 (EC50 = 0.080 μM), stabilizes hydrophobic core I of Aβ42 peptide (residues 17-21) to its α-helical conformation by interacting specifically in this region. [1] K01-162 shows full MC65 protection at 125 nM, an EC50 of 80 nM, and no cytotoxicity up to 50 μM. [2]in vivo:K01-162 can reduce the brain amyloid burden that exists in both fibrillar and RIPA-soluble, non-fibrillar forms.[2]
[1]. Li J, et al. Alzheimer's disease drug candidates stabilize A-β protein native structure by interacting with the hydrophobic core. Biophys J. 2011 Feb 16;100(4):1076-82. [2]. Hong HS, et al. Candidate anti-A beta fluorene compounds selected from analogs of amyloid imaging agents. Neurobiol Aging. 2010 Oct;31(10):1690-9.