BO-264 is a highly TACC3 inhibitor with IC50 value of 188nM. It significantly decreased centrosomal TACC3 during both mitosis and interphase, as well as displayed potent anti-proliferative activity (~90% have less than 1μM GI50 value) in the NCI-60 cell line panel compromising nine different cancer types.

KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).

KHS101 is a selective inducer of neuronal differentiation. It induced neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50 ~1 μM), suppressed astrocyte formation, and also induced acceleration of neuronal differentiation in the hippocampal dentate gyrus in vivo.