Related Experiment Video
Updated: Aug 11, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities
Pui-Kai Li1, Bulbul Pandit, Dan L Sackett
1Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210-1291, USA. li.27@osu.edu
Abstract:
We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro. Flow cytometric analyses showed that the compound caused G2-M arrest, which occurred mainly at the mitotic phase. In addition, immunofluorescence microscopy and in vitro tubulin polymerization studies showed that 5HPP-33 has antimicrotubule activity with a paclitaxel-like mode of action. It is effective against four different paclitaxel-resistant cell lines. Thus, 5HPP-33 represents a potential antitumor agent.
Related Concept Videos
Drugs that Stabilize Microtubules
Drugs that Destabilize Microtubules
Destabilization of Microtubules
Inhibition of Cdk Activity
Inhibition of CDK Activity
Anthelminthic Agents
