hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM)[1].
HSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with IC50 value <0.05 nM. hSMG-1 inhibitor 11e exhibits 900-fold selectivity for hSMG-1 over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50 of 61 nM and 92 nM) and CDK1/CDK2 (IC50 of 32 μM and 7.1 μM).
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.
| mTOR 45 nM (IC 50 ) | PI3Kα 61 nM (IC 50 ) | PI3Kγ 92 nM (IC 50 ) | CDK1 32 μM ( IC 50 ) | CDK2 7.1 μM (IC 50 ) | hSMG-1 <0.05 nM (IC 50 ) |
hSMG-1: <0.05 nM (IC50); mTOR: 45 nM (IC50); PI3Kα: 61 nM (IC50); PI3Kγ: 92 nM (IC50); CDK1: 32 μM (IC50); CDK2: 7.1 μM (IC50)
[1] Ariamala Gopalsamy, et al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41. DOI:
10.1016/j.bmcl.2012.08.107
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