1. Apoptosis
  2. MDM-2/p53
  3. LLQ-45

LLQ-45 是一种共价 p53Y220C 突变蛋白激动剂,其 EC50 为 24.97 μM。LLQ-45 可通过共价修饰激活 p53Y220C 的抗肿瘤功能,恢复其 DNA 结合能力并提高热稳定性。LLQ-45 可选择性抑制 p53Y220C 突变肿瘤细胞的增殖,抑制细胞生长并上调 CDKN1A 的表达。LLQ-45 可用于 p53Y220C 突变型癌症的相关研究。

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LLQ-45

LLQ-45 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LLQ-45 is a covalent p53Y220C mutant protein agonist with an EC50 of 24.97 μM. LLQ-45 activates the anti-tumor function of p53Y220C through covalent modification, restores its DNA-binding ability and enhances its thermal stability. LLQ-45 selectively inhibits the proliferation of p53Y220C mutant tumor cells, suppresses cell growth and upregulates the expression of CDKN1A. LLQ-45 can be used in studies related to p53Y220C mutant cancers[1].

体外研究
(In Vitro)

LLQ-45 (6 天) 相较 p53 野生型肿瘤细胞 (HUH-6、H1299-WT),可选择性抑制 p53Y220C 突变型肿瘤细胞 (HUH-7、H1299-Y220C) 的增殖,其 IC50 值分别为 1.35 μM、5.77 μM、2.92 μM 和 8.42 μM[1]
LLQ-45 (25-100 μM; 24 h) 可通过处理 24 小时后呈剂量依赖性上调 CDKN1A、PUMA 和 NOXA 的表达,选择性恢复 HUH-7 (p53Y220C) 细胞中 p53 的转录功能,而对 HUH-6 (p53 野生型) 细胞中的上述基因无影响[1]

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

Real Time qPCR[1]

Cell Line: HUH-7 (p53 Y220C mutant) hepatocellular carcinoma cells, HUH-6 (p53 wild-type) hepatocellular carcinoma cells
Concentration: 25 μM (24 h incubation); 50 μM (24 h incubation); 100 μM (24 h incubation)
Incubation Time: 24 h
Result: Induced significant, dose-dependent upregulation of CDKN1A, PUMA, and NOXA mRNA expression in HUH-7 cells.
Caused no appreciable induction of CDKN1A, PUMA, NOXA, or MDM2 in HUH-6 cells.
分子量

307.35

Formula

C17H17N5O

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)

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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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LLQ-45
目录号:
HY-182744
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