Blebbistatin is really a broadly used inhibitor of myosin 2 that allows study regarding an extensive selection of cytoskeleton-related processes. However, blebbistatin has lots of limitations hindering its applicability: it’s fluorescent, poorly water soluble, cytotoxic, and vulnerable to (photo)degradation. Despite these negative effects, to be the only accessible myosin 2-specific inhibitor, blebbistatin is quite a range of necessity. Blebbistatin continues to be modified to enhance its qualities and a few of the new compounds are actually helpful replacements from the original molecule. This review summarizes recent results on blebbistatin development. We discuss the medicinal perspectives of those efforts, as myosins have become promising drug target candidates for various conditions varying from neurodegeneration to muscle disease, wound healing, and cancer metastasis.