MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

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

MBM-55 (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells. MBM-55 (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.MBM-55 inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively[1].

In female BALB/c nu/nu mice bearing HCT-116 xenografts, MBM-55 (20 mg/kg; i.p.) exhibits good antitumor activity and a well-tolerated dose schedule. MBM-55 (1.0 mg/kg; i.v.) shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively[1].