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Cat. No.: 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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Formule: C₁₇H₁₇N₅O
Masse moléculaire:307.35

Stockage:

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

LLQ-45 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

In Vitro

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.

Chemical Information

Masse moléculaire 307.35
Formule C₁₇H₁₇N₅O
SMILES

C=C(C(N1C=CC2=C(N=CN=C21)C3=CN(N=C3)C4CCC4)=O)C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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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