1. Apoptosis
  2. MDM-2/p53 Apoptosis
  3. ADH-6

ADH-6 是一种三吡啶酰胺化合物。ADH-6 消除了突变 p53 DBD 的聚集成核亚结构域的自组装。ADH-6 靶向并解离人类癌细胞中的突变 p53 聚集体,从而恢复 p53 的转录活性,导致细胞周期停滞和细胞凋亡 (apoptosis)。ADH-6 具有研究癌症疾病的潜力。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 ADH-6 TFA 通常具有更好的水溶性和稳定性。

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ADH-6 Chemical Structure

ADH-6 Chemical Structure

CAS No. : 2227429-65-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].

体外研究
(In Vitro)

ADH-6 (25 μM, 10 h) inhibits aggregation of pR248W (indicated by dot blot assay)[1].
ADH-6 (5 μM, 6 h) dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells[1].
ADH-6 (0-10 μM, 24 or 48 h) causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2)[1].
ADH-6 (5 μM, 24 h) specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells[1].

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

Cell Viability Assay[1]

Cell Line: MIA PaCa-2 (mutant R248W p53), SK-BR-3 (mutant R175H p53)
Concentration: 0, 2.5, 5, 7.5, 10 μM
Incubation Time: 24, 48 h
Result: Caused death of cancer cells bearing mutant, but not WT, p53.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Increased expression of p53-inducible MDM2 and proapoptotic Bax.
体内研究
(In Vivo)

ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) causes regression of mutant p53-bearing tumors [1].

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

Animal Model: MIA PaCa-2 xenografts[1]
Dosage: 716.4 µM in 0.02% DMSO
Administration: Intraperitoneal injection, every 2 days, for a total of 12 doses
Result: Reduced tumor growth relative to the saline-treated control group.
Reduced mutant p53 levels and shrinked xenografts harboring aggregation-prone mutant p53.
Animal Model: MIA PaCa-2 xenografts (pharmacokinetics assay)[1]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection, for a single dose
Result: Cmax: 21 µg/mL, T1/2: 3.6 h
分子量

640.64

Formula

C29H36N8O9

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

ADH-6 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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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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ADH-6
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HY-145785
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