NBI-961

NBI-961 (also known as CMP3a) is a preclinical-stage, small-molecule, bifunctional inhibitor of NIMA-related kinase 2 (NEK2). It was originally discovered and patented by the University of Arizona and developed in collaboration with Synactix Pharmaceuticals, the University of Alabama at Birmingham, the University of Arkansas for Medical Sciences, and Xi'an Jiaotong University. NBI-961 exerts its antitumor effects through a dual mechanism: it catalytically inhibits NEK2 kinase activity and simultaneously induces its proteasome-mediated degradation. In preclinical models, NBI-961 has demonstrated potent efficacy against glioblastoma (GBM) by destabilizing the histone methyltransferase EZH2 and reversing radioresistance. Additionally, it has shown significant activity in diffuse large B-cell lymphoma (DLBCL) by inducing G2/M cell-cycle arrest and apoptosis, and sensitizing lymphoma cells to chemotherapeutic agents such as doxorubicin and vincristine.

Other names

(R)-5-{7-[1-(2-dimethylamino-ethyl)-1H-pyrazol-4-yl]-imidazo[1,2-a]pyridin-3-yl}-3-[1-(2-trifluoromethyl-phenyl)-ethoxy]-thiophene-2-carboxamidecompound 3acompound3acompound-3a