1. Apoptosis
  2. MDM-2/p53 Apoptosis
  3. UCI-LC0019

UCI-LC0019 是一种突变型 p53 再激活剂。UCI-LC0019 可结合突变型 p53,诱导类野生型构象变化,恢复序列特异性 DNA 结合活性,激活 p53 依赖性转录程序,且不通过巯基反应性或谷胱甘肽耗竭发挥作用。UCI-LC0019 可抑制携带突变型 p53 的癌细胞增殖并诱导细胞凋亡 (apoptosis),而对 p53null 或野生型 p53 肿瘤细胞无显著作用。UCI-LC0019 在携带 p53R175H 突变肿瘤的异种移植小鼠模型中表现出抗肿瘤活性。UCI-LC0019 可用于癌症研究,例如卵巢癌。

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UCI-LC0019

UCI-LC0019 Chemical Structure

CAS No. : 1372406-51-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer[1].

体外研究
(In Vitro)

UCI-LC0019 可强效抑制表达 p53G245S 的 Saos-2 细胞 (IC50 = 16.5 μM) 和表达 p53R175H 的 TOV112D 细胞 (IC50 = 15.2 μM) 的增殖,而对 p53null Saos-2 细胞的活性较低 (IC50 = 24.1 μM)[1]
UCI-LC0019 (0-30 μM; 3-72 h) 可快速降低表达 p53R175H 的 TOV112D 细胞的增殖能力并诱导其凋亡[1]
UCI-LC0019 (25-30 μM; 3 days) 可通过不依赖巯基反应性的机制抑制表达 p53R175H 的 TOV112D 细胞增殖,因为与 5 mM NAC (HY-B0215) 联合处理无法逆转其抗增殖作用[1]

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

Cell Proliferation Assay[1]

Cell Line: p53R175H-expressing TOV112D cells
Concentration: 30 μM
Incubation Time: 3, 12, 24 h
Result: Induced rapid cell death time-dependently.
体内研究
(In Vivo)

UCI-LC0019 (10 mg/kg;腹腔注射;每日 1 次,连续 10 天) 可抑制表达 p53R175H 的 TOV112D 异种移植瘤小鼠的肿瘤生长[1]

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

Animal Model: Mice with p53R175H-expressing TOV112D Xenografts[1]
Dosage: 10 mg/kg
Administration: i.p.; daily for 10 days
Result: Reduced tumor volume.
Increased GSH levels.
Did not result in weight loss or any obvious toxic effects.
分子量

278.31

Formula

C17H14N2O2

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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UCI-LC0019
目录号:
HY-186151
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