AMA-37 是Arylmorpholine 的类似物，是ATP 竞争性的DNA-PK 抑制剂，其IC50 值分别为0.27 μM (DNA-PK)、32 μM (p110α)、3.7 μM (p110β)、and 22 μM (p110γ)。
货号:ajcx38356
CAS:404009-46-7
分子式:C17H17NO3
分子量：283.32
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively[1][2].

AMA-37 inhbits PI3K poorly[2].AMA-37 (20 μM) reduces the ability of UCN-01, isogranulatimide, and debromohymenialdesine, but not caffeine, to overcome G2 arrest (Ρ< 0.05)[3].Inhibition of DNA-PK with AMA37 leads to radiosensitization[3].

[1]. Zachary A Knight, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.
[2]. Zachary A Knight, et al. Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold. Bioorg Med Chem. 2004 Sep 1;12(17):4749-59.
[3]. Christopher M Sturgeon, et al. Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage. Mol Cancer Ther. 2006 Apr;5(4):885-92.