Tubulin polymerization-IN-36

Tubulin polymerization-IN-36 is a tubulin polymerization inhibitor (IC50: 2.8 μΜ). Tubulin polymerization-IN-36 binds to the colchicine site of tubulin and inhibits colchicine binding. Tubulin polymerization-IN-36 can be used in the research of cancers, such as lymphomas[1].

Research Areas >> Cancer

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

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Tubulin polymerization[1]

Tubulin polymerization-IN-36 (compound 2e, 1 μΜ, 72 h) inhibits proliferation of lymphoma cells below 50%[1]. Tubulin polymerization-IN-36 (50 and 500 nM, 24-72 h) induces cell apoptosis and arrests cell in G2/M phase in VL51 and MINO cells[1]. Tubulin polymerization-IN-36 (5 μΜ) inhibits colchicine binding to tubulin by 88%[1]. Tubulin polymerization-IN-36 shows cytotoxicity against MCF-7 cells (IC50: 0.29 μΜ)[1]. Cell Proliferation Assay[1] Cell Line: VL51, MINO, HBL1, SU-DHL-10 cells. Concentration: 0-10 μΜ Incubation Time: 72 h Result: Inhibited cell proliferation to 38%, 0.8%, 7.1%, 30.5% at 1 μΜ, respectively. IC50s: 0.04, 0.02, 0.02, 0.03 μΜ, respectively. Cell Cycle Analysis[1] Cell Line: VL51 and MINO cells Concentration: 50 and 500 nM Incubation Time: 24, 48 and 72 h Result: Arrested cell in G2/M phase.

[1]. Michael D Wendt, et al. Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: Further chemical modifications and potential therapeutic effects against lymphomas. J Med Chem. 2006 Feb; 49(3): 1165-81.