1. Neuronal Signaling Stem Cell/Wnt
  2. Notch
  3. ATOX1-IN-1

ATOX1-IN-1 是一种 ATOX1 (一种铜伴侣蛋白) 抑制剂,Kd 为 12.5 μM。ATOX1-IN-1 诱导细胞内铜蓄积、提高 NOTCH1 启动子区域的 DNA 甲基化水平,并抑制 NOTCH1/HES1 信号通路。ATOX1-IN-1 可增强肝癌细胞对 Cisplatin (HY-17394) 的敏感性。ATOX1-IN-1 可用于肝癌相关研究。

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ATOX1-IN-1

ATOX1-IN-1 Chemical Structure

CAS No. : 956181-19-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATOX1-IN-1 is an inhibitor of ATOX1 (a copper chaperone protein) with a Kd value of 12.5 μM. ATOX1-IN-1 induces intracellular copper accumulation, increases the level of DNA methylation in the NOTCH1 promoter region, and inhibits the NOTCH1/HES1 signaling pathway. ATOX1-IN-1 enhances the sensitivity of hepatocellular carcinoma cells to Cisplatin (HY-17394). ATOX1-IN-1 can be used in hepatocellular carcinoma-related research[1].

体外研究
(In Vitro)

ATOX1-IN-1 (Compound 8) (48 h) 可抑制 HepG2 和 Huh7 肝癌细胞的活力,其 IC50 值分别为 16.5 μM 和 22.0 μM,且相较于永生化肝细胞 THLE-2 对癌细胞具有高选择性[1]
ATOX1-IN-1 (10 μM) 与 10 μM Cisplatin 联合使用时,对 HepG2 和 Huh7 肝癌细胞具有更显著的抗增殖和促凋亡效果[1]
ATOX1-IN-1 (5-15 μM) 可在体外以浓度依赖的方式抑制 HepG2 和 Huh7 肝癌细胞中的 NOTCH1/HES1 信号通路,降低 NOTCH1 和 HES1 的 mRNA 及蛋白表达水平[1]
ATOX1-IN-1 (5-15 μM) 以浓度依赖的方式升高 HepG2 和 Huh7 肝癌细胞内的铜水平[1]
ATOX1-IN-1 (5-15 μM) 以浓度依赖的方式在体外增强 HepG2 和 Huh7 肝癌细胞中 NOTCH1 启动子的 DNA 甲基化[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

ATOX1-IN-1 (10 mg/kg;腹腔注射;每日 1 次共 10 天) 在 HepG2 肝癌异种移植模型中表现出抗肿瘤活性,与 Cisplatin 联用时可产生具有协同作用且耐受性良好的抗肿瘤效果[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (6-8 weeks old, 18-22 g, equal male/female ratio, subcutaneous HepG2 xenograft model)[1]
Dosage: 10 mg/kg
Administration: i.p.; once daily for 10 days
Result: Reduced tumor volume and proliferation marker (Ki67, PCNA) expression compared to the control group.
Produced a significantly greater tumor inhibition effect when combined with cisplatin than either single agent, with the combination group showing the smallest tumor volume, lowest Ki67 and PCNA expression, and no obvious pathological changes in major organs (heart, liver, lung, kidney, gastrointestinal tract).
分子量

546.57

Formula

C33H26N2O6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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产品名称:
ATOX1-IN-1
目录号:
HY-181975
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