Drug intelligence / Profile preview

reversine

Development stage
Preclinical
Lead developer
Peter G. Schultz group
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Reversine is a synthetic small molecule purine derivative first synthesized in 2004 by the group of Peter G. Schultz. It functions as a potent inhibitor of several kinases, most notably Aurora kinases (A/B/C), Mps1 (monopolar spindle 1 kinase), and MEK1, and also acts as an antagonist at the adenosine A3 receptor. Reversine is widely used in research to study chromosome segregation and cell cycle regulation due to its ability to induce cell dedifferentiation and apoptosis, particularly in cancer cells. It has shown efficacy in preclinical models for inhibiting growth of various cancer cells through mechanisms such as G2/M phase arrest and mitochondria-independent apoptosis[1][3][4]. Reversine is not approved for clinical use but serves as a lead compound for potential antitumor agents.

Other names
2-(4-morpholinoanilino)-6-cyclohexylaminopurine
02

Targets

ADORA3 (Adenosine A3 receptor)AURKB (Aurora kinase B)AURKC (Aurora kinase C)AURKA (Aurora kinase A)TTK (TTK protein kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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