1. Apoptosis Cell Cycle/DNA Damage
  2. Ferroptosis Polo-like Kinase (PLK) MDM-2/p53
  3. L14-8

L14-8 是一种强效的铁死亡 (ferroptosis) 诱导剂。L14-8 通过泛素化作用促进 PLK1 的降解,增加 TP53 的磷酸化和 SAT1 的转录,从而引发铁死亡和癌细胞死亡。DNH28 可用于研究晚期前列腺癌。

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L14-8 Chemical Structure

L14-8 Chemical Structure

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查看 Polo-like Kinase (PLK) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L14-8 is a potent ferroptosis inducer. L14-8 promotes PLK1 degradation via ubiquitination, increasing TP53 phosphorylation to enhance SAT1 transcription, thereby triggering ferroptosis and cancer cell death. DNH28 can be used for the study of advanced prostate cancer[1].

体外研究
(In Vitro)

L14-8 (5-25 μM, 48 h) 在 C4-2B 和 22Rv1 细胞中均导致超过 80% 的细胞死亡,而在 25 μM 下对正常前列腺细胞的生长没有显著影响[1]
L14-8 (10 μM, 24-48 h) 通过转录激活 SAT1 表达,升高 MDA 水平的方式在 C4-2B 和 22Rv1 细胞中引发铁死亡[1]
L14-8 (0-10 μM, 0-24 h) 在 C4-2B 和 22Rv1 细胞中通过结合 PLK1 并增强 PLK1 介导的 TP53 磷酸化和表达,从而激活 SAT1 转录[1]

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

Cell Viability Assay[1]

Cell Line: C4-2B and 22Rv1 cells
Concentration: 5 and 7.5 μM
Incubation Time: 72 h
Result: Significantly rescued the inhibitory effect of L14-8 on the viability of C4-2B and 22Rv1 cells.
Significantly reduced the sensitivity of the cells after knocking out TP53.

RT-PCR[1]

Cell Line: C4-2B and 22Rv1 cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Dramatically increased the the expression of ferroptosis-related genes SAT1.

Western Blot Analysis[1]

Cell Line: C4-2B and 22Rv1 cells
Concentration: 0, 1, 2, 4, 8, 12 and 24 h
Incubation Time: 72 h
Result: Significantly increased the thermal stability of endogenous PLK1.
led to an increase in the protein levels of TP53 and phosphorylated TP53 (p-TP53) .
Significantly shortened the half-life of PLK1.
体内研究
(In Vivo)

L14-8 (10-20 mg/kg, i.p., 1 天 1 次,共 25 天) 在 C4-2B 肿瘤移植小鼠模型中,能够抑制前列腺肿瘤生长,且无明显毒性作用[1]

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

Animal Model: C4-2B cells xenografted model established in male 4-week-old BALB/c nude mice[1]
Dosage: 10 and 20 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 25 days
Result: Significantly suppressed tumor growth in a dose-dependent manner.
Decreased cancer proliferation.
Had no changes in major organs such as the heart, kidney, liver, lung, and spleen with high doses.
Had similar liver and kidney function indices between vehicle treatment in lower doses.
分子量

517.52

Formula

C30H25F2NO5

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
L14-8
目录号:
HY-175000
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