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

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.

For research use only. We do not sell to patients.

LLQ-45

LLQ-45 Chemical Structure

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Description

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].

In Vitro

LLQ-45 (6 days) selectively inhibits proliferation of p53Y220C 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 (p53Y220C) 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.
Molecular Weight

307.35

Formula

C17H17N5O

SMILES

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

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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  • 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
Cat. No.:
HY-182744
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