Indibulin

Indibulin (ZIO 301) , an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Research Areas >> Neurological Disease

Tubulin[1]

Indibulin (300-2100 nM; 48 hours) inhibits the proliferation of MCF-7 cells with an IC50 of 150 nM[1]. Indibulin (300, 600 nM; 48 hours) blockes the cells in the G2/M phase indicating that indibulin blockes the progression of the cell cycle at mitosis[1]. Indibulin (150-600 nM; 24 hours) induces apoptosis in MCF-7 cells[1]. Indibulin (150-600 nM; 48 hours) with 300 and 600 nM generates cleaved fragments of PARP protein the treatment of MCF-7 cells[1]. Cell Proliferation Assay[1] Cell Line: MCF-7 cells Concentration: 300, 600, 900, 1200, 1500, 1800, 2100 nM Incubation Time: 48 hours Result: Inhibited the proliferation of MCF-7 cells with an IC50 of 150 nM. Cell Cycle Analysis[1] Cell Line: MCF-7 cells Concentration: 300, 600 nM Incubation Time: 48 hours Result: Blocked the cells in the G2/M phase of the cell cycle. Apoptosis Analysis[1] Cell Line: MCF-7 cells Concentration: 150, 300 and 600 nM Incubation Time: 24 hours Result: Induced apoptosis in MCF-7 cells. Western Blot Analysis[1] Cell Line: MCF-7 cells Concentration: 150, 300 and 600 nM Incubation Time: 48 hours Result: Generated cleaved fragments of PARP protein in 300 and 600 nM.

[1]. Kapoor S, et al. Indibulin dampens microtubule dynamics and produces synergistic antiproliferative effect with vinblastine in MCF-7 cells: Implications in cancer chemotherapy. Sci Rep. 2018 Aug 17;8(1):12363.