TAI-1

TAI-1是一个有效的特异Hec1抑制剂，会打乱Hec1-Nek2蛋白质相互作用。 TAI-1 disrupts the binding of Nek2 to Hec1, which leads to degradation of Nek2 and chromosomal misalignment. TAI-1 shows strong growth inhibitory potency at nM levels across a broad spectrum of tumor cells, and produces synergistic activity with doxorubicin, topotecan and paclitaxel in leukemia, breast and liver cancer cells. TAI-1 (20 mg/kg i.v. or 150 mg/kg p.o.) causes significant tumor growth delay in Huh-7 model and modest tumor inhibition in Colo205 and MDA-MB-231 models.