2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. p53 Activator 17

p53 Activator 17 是一种 p53-Y220C 激活剂。p53 Activator 17 对 p53-Y220C 突变型癌细胞系表现出选择性细胞毒性和促凋亡 (apoptosis) 活性，而对野生型或 p53 缺失细胞的影响甚微。p53 Activator 17 可诱导细胞内 p53-Y220C 从突变型向野生型构象转变，并伴随经典 p53 靶基因，包括 BBC3 (PUMA) 和 MDM2 的转录激活。p53 Activator 17 可用于肝细胞癌和乳腺癌的研究。

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p53 Activator 17

p53 Activator 17 Chemical Structure

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p53 Activator 17 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer[1].

体外研究
(In Vitro)

p53 Activator 17 (Compound JC36) (60 μM，24 小时) 选择性地诱导 HUH7 细胞中 p53-Y220C 突变蛋白发生野生型构象变化，但对 MCF7 细胞中的野生型 p53 无影响[1]。
p53 Activator 17 (30-120 μM，48 小时) 选择性地抑制携带 p53-Y220C 突变的 HUH7 细胞、MCF7 细胞和其他细胞的活力[1]。
p53 Activator 17 (60 μM，48 小时) 显著增加 HUH7 p53-Y220C 细胞的凋亡[1]。
p53 Activator 17 (60 μM，24 小时) 显著增加 HUH7 p53-Y220C 和 MCF7 p53-Y220C 细胞中 p53 靶基因的表达[1]。
p53 Activator 17 (60 μM, 24 h) 可增加 MCF7 p53-Y220C 细胞中 p53 总蛋白水平；在 HUH7 p53-Y220C 和 MCF7 p53wt 细胞中未观察到显著变化[1]。

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

p53 Activator 17 相关抗体:

Apoptosis Analysis[1]

Cell Line: HUH7 p53-Y220C
Concentration: 60 μM
Incubation Time: 48 h
Result: Significantly increased apoptosis in HUH7 p53-Y220C cells (total apoptotic cells increased by approximately 14-fold).
Apoptosis was increased but not significantly in MCF7 p53-Y220C; apoptosis increased by 1.9-fold in MCF7 p53wt.

Real Time qPCR[1]

Cell Line: HUH7 p53-Y220C cells, MCF7 p53-Y220C cells
Concentration: 60 μM
Incubation Time: 24 h
Result: Significantly increased expression of C3 (PUMA) and MDM2 in HUH7 p53-Y220C cells.
Significantly increased expression of BBC3 and CDKN1A (p21) in MCF7 p53-Y220C.
In MCF7 p53wt, MDM2 expression was increased, but BBC3 expression remained unchanged.
分子量

333.23

Formula

C15H17BrN4
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

p53 Activator 17 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

Keywords:

p53 Activator 17MDM-2/p53Apoptosisp53-Y220Cmutant p53 reactivationapoptosis inductionindazole derivativesInhibitorinhibitorinhibit

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