AMA-37 |
| カタログ番号GC64818 |
アリールモルホリン類似体である AMA-37 は ATP 競合的 DNA-PK 阻害剤であり、IC50 値はそれぞれ 0.27 μM (DNA-PK)、32 μM (p110α)、3.7 μM (p110β)、および 22 μM (p110γ) です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 404009-46-7
Sample solution is provided at 25 µL, 10mM.
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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.
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