J-14
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- CAS号:
- 1043854-13-2
- 英文名:
- J-14
- 英文别名:
- 4-(((4-(4-(2-Chlorophenyl)piperazin-1-yl)-6-phenylpyrimidin-2-yl)thio)methyl)benzoic acid;Benzoic acid, 4-[[[4-[4-(2-chlorophenyl)-1-piperazinyl]-6-phenyl-2-pyrimidinyl]thio]methyl]-;cancer,inhibit,damage,Sulfiredoxin,J14,cytotoxicity,Reactive Oxygen Species,J 14,death,adenocarcinoma,Inhibitor,lung,mitochondrial,cells
- 中文名:
- J-14
- 中文别名:
- 化合物J-14;4-(((4-(4-(2-氯苯基)哌嗪-1-基)-6-苯基嘧啶-2-基)硫代)甲基)苯甲酸
- CBNumber:
- CB95559036
- 分子式:
- C28H25ClN4O2S
- 分子量:
- 517.04
- MOL File:
- 1043854-13-2.mol
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J-14化学性质
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沸点:
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762.9±60.0 °C(Predicted)
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密度:
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1.42±0.1 g/cm3(Predicted)
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储存条件:
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Sealed in dry,Room Temperature
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溶解度:
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DMSO: 260 mg/mL (502.86 mM)
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酸度系数(pKa):
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4.08±0.10(Predicted)
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J-14性质、用途与生产工艺
J14 是一种可逆 sulfiredoxin 抑制剂，IC50 为 8.1 μM。J14 通过抑制 sulfiredoxin 诱导氧化应激 (导致细胞内 ROS 积累)，从而导致细胞毒性和癌细胞死亡。
IC50: 8.1 μM (Sulfiredoxin); ROS
J14 (0-100 μM; 0-96 hours; A549 cells) treatment inhibits the growth of A549 cells in a concentration- and a time- dependent manner, and its half inhibitory concentration for the growth of A549 cells was 15.7 μM.
J14 (20 μM; 48-72 hours; A549 cells) treatment causes not only the release of cytochrome c into the cytosol, but also the activation of caspase-3 and caspase-9. J14 induces oxidative damage to mitochondria, resulting in caspase-mediated apoptosis.
J14 treatment significantly increases the accumulation of sulfinic peroxiredoxins and intracellular ROS. Excess accumulation of intracellular ROS causes oxidative damage, leading to cell death. J14 significantly induces cell death in A549 cells in a time-dependent manner, resulting in approximately 40% cell death in 96 hours.
J14 induces oxidative mitochondrial damage and apoptosis.
Cell Viability Assay
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Cell Line:
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A549 cells
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Concentration:
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0-100 μM
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Incubation Time:
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0 hour, 24 hours, 48 hours, 72 hours, 96 hours
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Result:
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Inhibited the growth of A549 cells in a concentration- and a time- dependent manner.
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Western Blot Analysis
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Cell Line:
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A549 cells
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Concentration:
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20 μM
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Incubation Time:
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48 hours, 72 hours
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Result:
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Caused not only the release of cytochrome c into the cytosol, but also the activation of caspase-3 and caspase-9.
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J14 (50 mg/kg; intraperitoneal injection; daily; for 16 days; BALB/c nude female mice) treatment significantly reduces the average tumor volume. The masses and weights of the primary tumors excised from the J14-treated mice are significantly lower compared with those of the control mice.
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Animal Model:
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Six-week-old BALB/c nude female mice injected with A549 cells
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Dosage:
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50 mg/kg
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Administration:
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Intraperitoneal injection; daily; for 16 days
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Result:
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Significantly reduced the growth of human lung tumor without acute toxicity.
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J-14
上下游产品信息
上游原料
下游产品
1043854-13-2, J-14 相关搜索:
- C28H25ClN4O2S
- 化合物J-14
- 4-(((4-(4-(2-氯苯基)哌嗪-1-基)-6-苯基嘧啶-2-基)硫代)甲基)苯甲酸
- 1043854-13-2
- cancer,inhibit,damage,Sulfiredoxin,J14,cytotoxicity,Reactive Oxygen Species,J 14,death,adenocarcinoma,Inhibitor,lung,mitochondrial,cells
- 4-(((4-(4-(2-Chlorophenyl)piperazin-1-yl)-6-phenylpyrimidin-2-yl)thio)methyl)benzoic acid
- Benzoic acid, 4-[[[4-[4-(2-chlorophenyl)-1-piperazinyl]-6-phenyl-2-pyrimidinyl]thio]methyl]-