MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

RSK1:5.4 nM , Akt1:608 nM , GSK-3β:91 nM , NEK2:1 nM , CDK2:370 nM , Abl:20 nM , CDK4:441nM , DYRK1A:6.5 nM , Chk1:57 nM , Aurora A:5300 nM

MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 and DYRK1a with IC50s of 5.4 and 6.5 nM. MBM-55S inhibits MGC-803, HCT-116, and Bel-7402 the proliferation of cell with IC50s of 0.53, 0.84, and 7.13 μM, respectively. MBM-55S (0.5-1 μM) induces G2/M phase arrest and accumulation of cells with >4N content and causes cell apoptosis in a concentration-dependent manner in HCT-116 cells[1].

In female BALB/c nu/nu mice, MBM-55S (20 mg/kg; i.p) exhibits good antitumor activity. In male Sprague Dawley rats, MBM-55S (1.0 mg/kg; i.v.) shows good pharmacokinetic profile with the CL, T1/2, Vss, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 1.72 hours, 2.53 L/kg, 495 ng/h/mL and 507 ng/h/mL, respectively[1].