Reversine (656820-32-5) Description
Reversine is a small molecule developed by the group of Peter G. Schultz, used for stem cell dedifferentiation. Reversine is also a novel Aurora kinases inhibitor that inhibits colony formation of human acute myeloid leukemia cells. Reversine inhibits the phosphorylation of histone H3, a direct downstream target of Aurora kinases. Similarly to the Aurora kinase inhibitor VX-680, reversine inhibited colony formation of leukemic cells from patients with acute myeloid leukemia but was significantly less toxic than VX-680 on cells from healthy donors.
Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Reversine is a potent inhibitor of Aurora A and B and is also an inhibitor of Aurora C kinase. Aurora A and B activities are inhibited by 80% and Aurora kinase C by 55%, already at a concentration of 0.5 μM, whereas no inhibition or only modest inhibition is observed on others kinases tested. In a second round of experiments, the IC50 of Reversine is determined on Aurora kinase A to be 400 nM, whereas Aurora kinase B and C IC50 are 500 and 400 nM, respectively. The IC50 is also determined on MEK1 is >1.5 μM and that the IC50 on muscle myosin (an analogue of nonmuscle myosin II) is 350 nM.
Reversine (656820-32-5) Specifications
|Monoisotopic Mass||393.22771 g/mol|
|Solubility||Soluble in DMSO (~7-10 mg/ml)|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||A small synthetic purine analogue (2,6-disubstituted purine)|