p53 Activator 7

• CAT Number: I042483
• CAS Number: 2849340-59-4
• Molecular Formula: C27H32F3N4OP
• Molecular Weight: 516.54
• Purity: ≥95%
• Synonyms: 2-[3-(4-dimethylphosphorylanilino)prop-1-ynyl]-N-(1-methylpiperidin-4-yl)-1-(2,2,2-trifluoroethyl)indol-4-amine
• InChI: InChI=1S/C27H32F3N4OP/c1-33-16-13-21(14-17-33)32-25-7-4-8-26-24(25)18-22(34(26)19-27(28,29)30)6-5-15-31-20-9-11-23(12-10-20)36(2,3)35/h4,7-12,18,21,31-32H,13-17,19H2,1-3H3
• InChIKey: TWHPNHHZQSJOEI-UHFFFAOYSA-N
• SMILES: CN1CCC(CC1)NC2=C3C=C(N(C3=CC=C2)CC(F)(F)F)C#CCNC4=CC=C(C=C4)P(=O)(C)C

p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1)[1]. p53 Activator 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
The p53 protein, referred to as the “guardian of the human genome” , is a tetrameric transcription factor that prevents mutation to the genome by regulating the expression of a subgroup of target genes. Although biologically active as a homotetramer, each p53 monomer is comprised of 393 amino acids, and is divided into five key regulatory domains: the transactivation domain (TAD) , proline-rich region (PR) , the DNA binding domain (DBD) , the oligomerization domain (OD) , and the C-terminus[1].

Reference

[1]. Sujing LI, et al. Compounds targeting y220c mutant of p53. WO2022213975A1.