Alzheimer's disease (AD) is a neurodegenerative disorder that severely jeopardizes the health of aging populations all over the world. According to the amyloid cascade hypothesis, the pathological progression of AD is associated with the formation of amyloid plaques in the brain, resulting from the aggregation of amyloid-β (Aβ) peptides. Over the past few years, vast efforts have been dedicated to the development of amyloid probes and inhibitors for the diagnosis and effective treatment of AD. We review here recent advancements in luminescent probes for the detection of Aβ peptide and fibrils, and the current development of small molecule inhibitors of Aβ aggregation. We also highlight the key features in each specific example, as well as review new ideas and strategies that are crucial for researchers in this field.