hSMG-1 inhibitor 11e 是一种有效的选择性的 hSMG-1 激酶抑制剂，其 IC50 值<0.05 nM。hSMG-1 inhibitor 11e 对 hSMG-1 的选择性比 mTOR (IC50 为 45 nM)，PI3Kα/γ (IC50 为 61 nM 和 92 nM) 和 CDK1/CDK2 (IC50 为 32 μM 和 7.1 μM) 高 900 倍。
货号:ajcx33988
CAS:1402452-10-1
分子式:C26H27N7O3S
分子量：517.6
溶解度:DMSO : 50 mg/mL (96.60 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of 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 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[1].

[1]. Ariamala Gopalsamy, et al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.