Reversine is a cell-permeable, 2,6-disubstituted purine analog that acts as a dedifferentiation-inducing agent. Reversine is shown to induce mouse C2C12 myoblast cells to become multipotent mesenchymal progenitor cells in the concentration range of 1-10 M. Reversine is also the first organic molecule that has been demonstrated to reverse the cellular differentiation process. The compound acts as a selective A3 adenosine receptor antagonist (Ki= 660 nM, >10 M, and >10 M for hA3, hA1, and hA2A, respectively. Reversine functions as a dual inhibitor of MEK1 and nonmuscle myosin II heavy chain (IC50 = 8 and 10 nM, respectively). The compound also acts as an ATP-competitive, reversible and selective inhibitor of ARK-1, ARK-2, and ARK-3 (IC50 = 400, 500 and 400 nM, respectively) in a 26-kinase panel.
