hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC 50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC 50 of 45 nM), PI3Kα/γ (IC 50 s of 61 nM and 92 nM) and CDK1/CDK2 (IC 50 s of 32 μM and 7.1 μM)
In Vitro
hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.