Dysregulation of the activity of protein kinases has been associated with numerous diseases such as cancer or chronic inflammatory conditions. Therefore, protein kinases are attractive drug targets that are the most intensively pursued by both industrial and academic laboratories, with great success in the cancer field. Today, more than 40 protein kinase inhibitors have been approved for cancer therapy. This success, coupled with a greater understanding of inflammatory signalling cascades and cell death and regeneration pathways, led to kinase inhibitors taking centre stage in the pursuit for new drugs for the treatment of many unmet diseases. Moreover, considering that multiple sclerosis (MS) is classified as an autoimmune disease of the central nervous system (CNS), protein kinases as key drivers of many inflammatory-mediated diseases represent an important and promising class of emerging therapeutic targets for MS. It is only a matter of time to witness whether the modulation of the protein kinases collected in this chapter may become a valuable option for the future treatment of MS.