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製品番号: HY-182744

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LLQ-45

LLQ-45 is a covalent p53^Y220C mutant protein agonist with an EC₅₀ of 24.97 μM. LLQ-45 activates the anti-tumor function of p53^Y220C through covalent modification, restores its DNA-binding ability and enhances its thermal stability. LLQ-45 selectively inhibits the proliferation of p53^Y220C mutant tumor cells, suppresses cell growth and upregulates the expression of CDKN1A. LLQ-45 can be used in studies related to p53^Y220C mutant cancers.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₇H₁₇N₅O
分子量:307.35

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

LLQ-45 構造式

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Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

体外実験

LLQ-45 (6 days) selectively inhibits proliferation of p53^Y220C mutant tumor cells (HUH-7, H1299-Y220C) over p53 wild-type tumor cells (HUH-6, H1299-WT), with IC₅₀ values of 1.35 μM, 5.77 μM, 2.92 μM, and 8.42 μM respectively^[1].
LLQ-45 (25-100 μM; 24 h) selectively restores p53 transcriptional function in HUH-7 (p53^Y220C) cells by dose-dependently upregulating CDKN1A, PUMA, and NOXA expression after 24 h of treatment, with no effect on these genes in HUH-6 (p53 wild-type) cells^[1].

MedChemExpress (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.

化学情報

分子量 307.35
分子式 C₁₇H₁₇N₅O
SMILES

C=C(C(N1C=CC2=C(N=CN=C21)C3=CN(N=C3)C4CCC4)=O)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Li L, et al. Discovery of novel covalent agonists for p53 Y220C through synergistic strategy combining covalent binding and scaffold hopping. Eur J Med Chem. Published online March 31, 2026. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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