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ATN-224 (bis(choline)tetrathiomolybdate) is an orally active Cu2+/Zn2+-dependent superoxide dismutase 1 (SOD1) inhibitor used in research to modulate copper-dependent enzymatic activity and angiogenesis. It inhibits SOD1 activity in endothelial and tumor cells and has been characterized in cellular and in vivo models.
Orally active Cu2+/Zn2+ SOD1 inhibitor with reported IC50 ~17.5 nM in endothelial cells.
High affinity copper binder, showing selectivity against Ca, Fe, Mg, Zn, and Mn up to 1 mM.
Inhibits proliferation of HUVEC cells (IC50 ~1.4 μM) and purified SOD1 (IC50 ~0.33 μM after 24 h).
Time-dependent SOD1 inhibition, reaching maximal effect at ~16 hours.
Demonstrated inhibition of angiogenesis in Matrigel plug models in mice.
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