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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 266 | 现货 | |
2 mg | ¥ 378 | 现货 | |
5 mg | ¥ 579 | 现货 | |
10 mg | ¥ 928 | 现货 | |
25 mg | ¥ 1,790 | 现货 | |
50 mg | ¥ 2,980 | 现货 | |
100 mg | ¥ 4,770 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 637 | 现货 |
产品描述 | 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. |
靶点活性 | SOD1 (endothelial cells):17.5±3.7 nM |
体外活性 | 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. |
体内活性 | Inhibition of angiogenesis when ATN-224 is given by oral gavage occurred before there is measurable depletion of copper in either plasma or copper from the Matrigel plug. ATN-224 also significantly (P<0.05) inhibits angiogenesis in the Matrigel plug model in mice either when added directly to the plug or when given by oral gavage. This result shows that ATN-224 inhibits angiogenesis independently of copper depletion[1]. |
别名 | 四硫钼酸二胆碱, Bis(choline)tetrathiomolybdate |
分子量 | 432.56 |
分子式 | C10H28MoN2O2S4 |
CAS No. | 649749-10-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (115.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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