922150-11-6
Chemical Structure
SCH529074
- CAS No.: 922150-11-6
- Formula:C31H36Cl2N6
- Molecular Weight:563.56
IUPAC Name: N1-(2-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine
InChIKey: NCAJLQDPTZBGJV-UHFFFAOYSA-N
SMILES: CN(C)CCCNC1=C2C=CC=CC2=NC(CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)=N1
Biological Activity: SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC)[1][2].
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SCH529074 | 99.73% | SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC). | ||||||||||||||||||||
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- [1]. Miljana Nenkov, et al. Growth Inhibitory Role of the p53 Activator SCH 529074 in non‑small Cell Lung Cancer Cells Expressing Mutant p53. Oncol Rep. 2020 Jun;43(6):2073-2082. [Content Brief]
- [2]. Mark Demma, et al. SCH529074, a Small Molecule Activator of Mutant p53, Which Binds p53 DNA Binding Domain (DBD), Restores Growth-Suppressive Function to Mutant p53 and Interrupts HDM2-mediated Ubiquitination of Wild Type p53. J Biol Chem. 2010 Apr 2;285( [Content Brief]
Keywords
