Aftin-4 is an inducer of amyloid-β (1-42) (Aβ42).1 It selectively increases extracellular Aβ42 over Aβ40 production in N2a-AβPP695 cells when used at concentrations ranging from 1 to 100 mM. In vivo, aftin-4 (3-20 nmol/animal, i.c.v.) increases hippocampal Aβ42 content, lipid peroxidation, and production of the pro-inflammatory cytokines IL-1β, IL-6, and TNF-α in mice.2 It also induces spatial working and spatial reference memory deficits in mice, effects that are reversed by co-administration of the γ-secretase inhibitor BMS-299,897.
1.Hochard, A., Oumata, N., Bettayeb, K., et al.Aftins increase amyloid-β42, lower amyloid-β38, and do not alter amyloid-β40 extracellular production in vitro: Toward a chemical model of Alzheimer's disease?J. Alzheim. Dis.35(1)107-120(2013) 2.Meunier, J., Borjini, N., Gillis, C.N., et al.Brain toxicity and inflammation induced in vivo in mice by the amyloid-β forty-two inducer aftin-4, a roscovitine derivativeJ. Alzheim. Dis.44(2)507-524(2015)