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    ATN-224抑制剂、激动剂

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    ATN-224抑制剂、激动剂

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      • 货号:

        YZJ3836

      • 规格:

        649749-10-0

      ATN-224抑制剂、激动剂(CAS号649749-10-0)ATN-224(tetrathiomolybdate)是铜螯合剂,能抑制细胞内的SOD1活性,IC50为17.5 nM。 ATN-224(tetrathiomolybdate) is a copper-chelator agent which can inhibit intracellular SOD1 activity with IC50 of 17.5 nM.
      IC50 value: 17.5 nM [1]
      Target: SOD1
      in vitro: ATN-224 inhibits superoxide dismutase 1 (SOD1) in tumor and endothelial cells. The inhibition of SOD1 leads to inhibition of endothelial cell proliferation in vitro and attenuation of angiogenesis in vivo. The inhibition of SOD1 activity in endothelial cells is dose and time dependent and leads to an increase in the steady-state levels of superoxide anions, resulting in the inhibition of extracellular signal-regulated kinase phosphorylation without apparent induction of apoptosis [1]. ATN-224 (choline tetrathiomolybdate) can induce cell death in oxidative stress-resistant cells and cells overexpressing Bcl-2 by modulating the cellular redox environment and causing mitochondrial dysfunction. ATN-224 treatment decreases superoxide dismutase 1 (SOD1) activity, increases intracellular oxidants, and induces peroxynitrite-dependent cell death. ATN-224 also targets the mitochondria, decreasing both cytochrome c oxidase (CcOX) activity and mitochondrial membrane potential [2]. Treatment of HUVEC with ATN-224 caused increased superoxide levels, phospho-ERK signalling, nuclear NRF1 expression, HO-1 expression and induction of the anti-apoptotic proteins P21, BCL2 and BCLXL [4].
      in vivo: Low-dose ATN-224 (30 mg daily) may have biologic activity in men with biochemically-recurrent prostate cancer, as suggested by an improvement in PSA kinetics. However, the clinical significance of PSA kinetics changes in this patient population remains uncertain [3].
       
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