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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
5 mg | $64 | In Stock | |
10 mg | $109 | In Stock | |
25 mg | $218 | In Stock | |
50 mg | $372 | In Stock | |
100 mg | $596 | In Stock | |
1 mL x 10 mM (in DMSO) | $71 | In Stock |
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]. |
Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (115.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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