ATN-224

SKU: orb1308631

Description

ATN-224 (Bis(choline)tetrathiomolybdate) is an orally bioavailable, potent inhibitor of Cu/Zn-superoxide dismutase 1 (SOD1). It exhibits dose-dependent inhibition of SOD1 activity in endothelial cells with an IC50 of 17.5±3.7 nM. This small molecule is utilized in research exploring oxidative stress mechanisms, angiogenesis, and in models of cancer and neurodegenerative diseases.

Research Area

Metabolism Research

Key Properties

• CAS Number: 649749-10-0
• MW: 432.56
• Purity: 99.45% (May vary between batches)
• Formula: C₁₀H₂₈MoN₂O₂S₄
• SMILES: S=[Mo]([S-])([S-])=S.OCC[N+](C)(C)C.OCC[N+](C)(C)C
• Target: Others
• Solubility: DMSO:50 mg/mL (115.59 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.62 mM)

Bioactivity

• Target IC50:
  SOD1 (endothelial cells):17.5±3.7 nM
• In Vivo:
  Oral administration of ATN-224 leads to the inhibition of angiogenesis before any measurable reduction in copper levels in either plasma or the Matrigel plug is observed. Moreover, ATN-224 significantly (P<0.05) suppresses angiogenesis in the Matrigel plug model in mice, regardless of whether it is directly added to the plug or administered orally. These findings indicate that ATN-224's anti-angiogenic effects are not dependent on the depletion of copper.
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• In Vitro:
  ATN-224 is an orally-available inorganic small molecule that inhibits the copper/zinc-dependent enzyme, superoxide dismutase 1 (Cu/Zn-SOD1), in endothelial and tumor cells amd it is able to inhibit SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 inhibits FGF-2-induced ERK1/2 phosphorylation in a dose-dependent and time-dependent manner with an IC50 between 1.25 and 2.5 μM, consistent with the IC50 for the inhibition of proliferation, and it inhibits the proliferation of both HUVEC (IC50=1.4±0.3 μM; n=5) and it is also able to inhibit the activity of purified bovine SOD1 with an IC50 of 0.33±0.03 μM after 24 hours of incubation. ATN-224 has a specific and high affinity for copper ions (108 mol/L-1) and shows no binding to calcium, iron, magnesium, zinc, or manganese ions at concentrations up to 1 mM as determined by isothermal titration calorimetry. The SOD1 inhibition by ATN-224 is time dependent, reaching maximal inhibition at ~16 hours. ATN-224 seems to inhibit SOD1 by depleting the enzyme of copper.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SOD1, ATN 224, ATN224, ATN-224, Bis(choline)tetrathiomolybdate

Compound Identifiers

PubChem CID

18442052