ON 01500 is a tubulin inhibitor with a K d of 21 nM. ON 01500 exerts microtubule-destabilizing effects in cells. ON 01500 can be used the study of cancers [1] [2].
In Vitro, ON 01500 (1 μM) completely inhibits tubulin polymerization in MAP-rich tubulin samples[1]. ON 01500 (7-15 nM, 3-5 days) sensitizes cells to knockdown of TACC3 or overexpression of KIF2C and protects cells from overexpression of TACC3 or knockdown of KIF2C, with high toxicity[2]. ON 01500 (10 nM, 3-7 days) induces enrichment of L240F TUBB-expressing (mCherry-positive) K562 cells relative to wild-type cells[2].
References:
[1]. Baker SJ, et al. A Contaminant Impurity, Not Rigosertib, Is a Tubulin Binding Agent. Mol Cell. 2020 Jul 2;79(1):180-190.e4.
[2]. Jost, Marco et al. Pharmaceutical-Grade Rigosertib Is a Microtubule-Destabilizing Agent. Molecular Cell, Volume 79, Issue 1, 191 - 198.e3
In Vitro, ON 01500 (1 μM) completely inhibits tubulin polymerization in MAP-rich tubulin samples[1]. ON 01500 (7-15 nM, 3-5 days) sensitizes cells to knockdown of TACC3 or overexpression of KIF2C and protects cells from overexpression of TACC3 or knockdown of KIF2C, with high toxicity[2]. ON 01500 (10 nM, 3-7 days) induces enrichment of L240F TUBB-expressing (mCherry-positive) K562 cells relative to wild-type cells[2].
References:
[1]. Baker SJ, et al. A Contaminant Impurity, Not Rigosertib, Is a Tubulin Binding Agent. Mol Cell. 2020 Jul 2;79(1):180-190.e4.
[2]. Jost, Marco et al. Pharmaceutical-Grade Rigosertib Is a Microtubule-Destabilizing Agent. Molecular Cell, Volume 79, Issue 1, 191 - 198.e3