Drug intelligence / Profile preview

monastrol

Development stage
Preclinical
Lead developer
Harvard Medical School
Modality
Small Molecules
01

Overview

Monastrol is a cell-permeable small molecule that acts as a reversible and selective inhibitor of the mitotic kinesin Eg5 (also known as KIF11 or kinesin‑5), a motor protein essential for spindle bipolarity during mitosis. By binding to an allosteric site unique to Eg5 family members and inhibiting its ATPase activity, monastrol disrupts proper spindle formation and arrests cells in mitosis without interacting with tubulin. It was discovered by Thomas U. Mayer in Tim Mitchison’s lab and has been widely used as a research tool to probe mechanisms of cell division[2][5][7].

Other names
ethyl (4S)-4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate5-pyrimidinecarboxylic acid, 1,2,3,4-tetrahydro-4-(3-hydroxyphenyl)-6-methyl-2-thioxo-, ethyl ester, (4S)-Pilocereine ethyl etherCHEBI:75384UNII-6BSM97YZ8GUNII6BSM97YZ8GUNII 6BSM97YZ8GCAS 254753–54–3
02

Targets

KIF11 (Kinesin Spindle Protein)

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