PCC0208017 is a microtubule affinity regulating kinases ( MARK3/MARK4 ) inhibitor with IC 50 s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC 50 s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis . PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.