T-1101 tosylate (TAI-95 tosylate) is a potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).

CCT241950 (CCT 241950) is a small molecule NEK2 inhibitor, induces Tyr70Nek2 to jut into the ADP-binding pocket.

TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.

A potent, relatively selective Nek2 inhibitor with IC50 of 82.74 nM in cell-free assays; inhibits only 3 kinases (YSK4, FLT3-ITDD835V and FLT3-ITDF691L) against 97 kinases with >65% inhibition at 15 nM; blocks NEK2-EZH2 complex formation and inhibits tumor cell proliferation; efficiently attenuates GBM growth in mouse model and exhibits a synergistic effect with radiotherapy.

A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.67 uM; displays >10-fold selectivity over CDK2.

INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.

INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.