hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC 50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC 50 =50 nM), PI3Kα/γ (IC 50 =92/60 nM) and CDK1/CDK2 (IC 50 =32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
性状
Solid
IC50 & Target[1][2]
hSMG-1 0.11 nM (IC50) mTOR 50 nM (IC5
体外研究(In Vitro)
hSMG-1 inhibitor 11j (0.3-3 μM; 6 h) significantly reduces UPF1 phosphorylation at 0.3 μM, and eliminates it at 1 μM in MDA 361 cells.hSMG-1 inhibitor 11j inhibits MDA468 cell proliferation, with an IC50 of 75 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Gopalsamy A, et, al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.
溶解度数据
In Vitro: DMSO : 80 mg/mL (141.33 mM; Need ultrasonic)配制储备液