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TPEN

CAS No. : 16858-02-9

MCE 站：TPEN

产品活性：TPEN (TPEDA) 是一种特定的细胞可渗透的重金属螯合剂。TPEN 对 Zn²⁺ 具有高亲和力，但对 Mg²⁺ 和 Ca²⁺ 具有较低的亲和力。TPEN 诱导 DNA 损伤并增加细胞内 ROS 的产生。TPEN 还抑制细胞增殖并诱导凋亡 (apoptosis)。

研究领域：Immunology/Inflammation  |  NF-κB  |  Metabolic Enzyme/Protease  |  Apoptosis  |  Autophagy

作用靶点：Reactive Oxygen Species  |  Apoptosis  |  Autophagy

In Vitro: Heavy metal chelator TPEN attenuates fura-2 fluorescence changes induced by cadmium, mercury and methylmercury. TPEN, a cell-permeable chelator for heavy metal cations with a low affinity for Ca²⁺. In cells stimulated with 10 or 30 μM cadmium chloride, the addition of TPEN at 3 hr after exposure significantly decreases the elevated fura-2 fluorescence ratio to the basal levels within 10 min (119.6±2.4% or 109±1.5% decrease in ΔRatio (F340/F380) induced by 10 or 30 μM cadmium chloride, respectively), suggesting that a cadmium chloride-induced increase in the fura-2 fluorescence ratio is dependent on an increase in intracellular heavy metal cations but not intracellular Ca²⁺. TPEN is a metal chelator, which targets colon cancer cells through redox cycling of copper. TPEN reduces cell viability in a dose- and time-dependent manner. TPEN-induced cell death is also dependent on the redox cycling of copper since the copper chelator neocuproine inhibited DNA damage and reduced pChk1, γ-H2AX, and ATM protein expression. Cell death by low TPEN concentrations, involved ATM/ATR signaling in all 3 cell lines, since pre-incubation with specific inhibitors of ATM and DNA-PK led to the recovery of cells from TPEN-induced DNA damage.

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