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AMA-37

Names

[ CAS No. ]:
404009-46-7

[ Name ]:
AMA-37

[Synonym ]:
AMA37
ArylMorpholine Analog 37
1-(2-Hydroxy-4-morpholin-4-yl-phenyl)-phenyl-methanone
DNA-PK Inhibitor V

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> DNA-PK
Signaling Pathways >> PI3K/Akt/mTOR >> DNA-PK

[Target]

IC50: 0.27 μM (DNA-PK)[1].


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H17NO3

[ Molecular Weight ]:
283.32200

[ Exact Mass ]:
283.12100

[ PSA ]:
49.77000

[ LogP ]:
2.52480

[ Storage condition ]:
-20℃

Related Compounds