RGN6024

RGN6024 is an orally active, reversible small molecule that can penetrate the blood-brain barrier and acts as a microtubule (tubulin) destabilizer. It inhibits microtubule polymerization in both biochemical and cellular assays. RGN6024 binds to the colchicine-binding site of ?-tubulin with affinity constants of Kd= 6.7 ?M (SPR) and Kd= 7.4 ?M (tryptophan assay), inducing G2/M phase arrest in glioblastoma (GB) cells. The compound remains effective in cells overexpressing ?III-tubulin. Additionally, RGN6024 is able to suppress tumor growth in glioblastoma (GB) xenograft mouse models. This compound is applicable for research in glioblastoma (GB) .