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ATN-224

Catalog No. T14341   CAS 649749-10-0
Synonyms: Bis(choline)tetrathiomolybdate

ATN-224 (Bis(choline)tetrathiomolybdate) inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor.

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ATN-224 Chemical Structure
ATN-224, CAS 649749-10-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 76.00
2 mg In stock $ 106.00
5 mg In stock $ 156.00
10 mg In stock $ 225.00
25 mg In stock $ 405.00
50 mg In stock $ 590.00
100 mg In stock $ 859.00
1 mL * 10 mM (in DMSO) In stock $ 167.00
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Purity: 99.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ATN-224 (Bis(choline)tetrathiomolybdate) inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor.
Targets&IC50 SOD1 (endothelial cells):17.5±3.7 nM
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[2] 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[1], 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.
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[1].
Synonyms Bis(choline)tetrathiomolybdate
Molecular Weight 432.56
Formula C10H28MoN2O2S4
CAS No. 649749-10-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (115.59 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Juarez JC, et al. Copper binding by tetrathiomolybdate attenuates angiogenesis and tumor cell proliferation through the inhibition of superoxide dismutase 1. Clin Cancer Res. 2006 Aug 15;12(16):4974-82. 2. Lin J, et al. A non-comparative randomized phase II study of 2 doses of ATN-224, a copper/zinc superoxide dismutase inhibitor, in patients with biochemically recurrent hormone-naïve prostate cancer. Urol Oncol. 2013 Jul;31(5):581-8.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Inhibitor Library Clinical Compound Library Bioactive Compound Library Cuproptosis Compound Library Orally Active Compound Library Bioactive Compounds Library Max NO PAINS Compound Library

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Keywords

ATN-224 649749-10-0 Others ATN224 ATN 224 Bis(choline)tetrathiomolybdate inhibitor inhibit

 

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