1. Apoptosis
  2. MDM-2/p53
  3. UCI-1014

UCI-1014 is a mutant p53 (p53R175H) corrector/reactivator. UCI-1014 restores the wild-type-like DNA-binding activity of p53R175H, promotes the redistribution of the mutant protein to chromatin, and induces the expression of p53-dependent target genes. UCI-1014 inhibits the proliferation of p53R175H-mutant cancer cells through an SLC7A11-independent mechanism. UCI-1014 can be used for research related to p53-mutant cancers.

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

UCI-1014

UCI-1014 Chemical Structure

CAS No. : 304896-41-1

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Description

UCI-1014 is a mutant p53 (p53R175H) corrector/reactivator. UCI-1014 restores the wild-type-like DNA-binding activity of p53R175H, promotes the redistribution of the mutant protein to chromatin, and induces the expression of p53-dependent target genes. UCI-1014 inhibits the proliferation of p53R175H-mutant cancer cells through an SLC7A11-independent mechanism. UCI-1014 can be used for research related to p53-mutant cancers[1].

In Vitro

UCI-1014 (72 h) inhibits the proliferation of TOV-112D cells carrying p53R175H with an IC50 of 4.5 μM[1].
UCI-1014 (10-30 μM; 3 h) restores the DNA-binding ability of p53R175H in TOV-112D cells, and evidence shows that this mutant protein redistributes to the chromatin fraction after treatment with 10 μM or 30 μM for 3 hours[1].
UCI-1014 (3 h) induces p53-dependent gene expression in TOV-112D cells, with a transcriptome profile highly similar to that of UCI-1001, and it induces a greater number of p53-dependent genes after 3 hours of treatment[1].
UCI-1014 (5-20 μM; 72 h) exhibits growth inhibitory activity against TOV-112D cells, and this activity can only be partially reversed by 5 mM N-acetylcysteine (HY-B0215), indicating that its mechanism of action differs from that of thiol-reactive compounds such as APR-246 (HY-19980)[1].

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

Cell Viability Assay[1]

Cell Line: TOV-112D (p53-R175H)
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 72 h
Result: Had growth-inhibitory effects that were partially alleviated by 5 mM N-acetylcysteine at lower concentrations, but this mitigation diminished at 20 μM.
Molecular Weight

296.28

Formula

C16H12N2O4

CAS No.
SMILES

CC1=CC=C(C=C1)C2=CC=C(O2)/C=C3C(NC(NC\3=O)=O)=O

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