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 beta-tubulin with affinity constants of Kd= 6.7 µM (SPR) and Kd= 7.4 µM (tryptophan assay), inducing G2/M phase arrest in glioblastoma (GB) cells. The compound remains effective in cells overexpressing betaIII-tubulin. Additionally, RGN6024 is able to suppress tumor growth in glioblastoma (GB) xenograft mouse models. This compound is applicable for research in glioblastoma (GB).
Molecular Weight:
403.46
CAS Number:
[3055038-20-2]
Formula:
C18H21N5O4S
Target:
Microtubule Associated
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