PK11007, CAS [[874146-69-7]]

Artikelnummer: FBM-10-4176
Artikelname: PK11007, CAS [[874146-69-7]]
Artikelnummer: FBM-10-4176
Hersteller Artikelnummer: 10-4176
Alternativnummer: FBM-10-4176-5MG, FBM-10-4176-25MG
Hersteller: Focus Biomolecules
Kategorie: Biochemikalien
Alternative Synonym: Chemical Name: 5-Chloro-2-[(4-fluorophenyl)methylsulfonyl]-N-(5-methyl-1,3,4-thiadiazol-2-yl)pyrimidine-4-carboxamide
Reactivator of mutant p53
Molekulargewicht: 427.85
Reinheit: >98% by HPLC NMR (Conforms)
Formulierung: White solid
CAS Nummer: [874146-69-7]
Formel: C15H11ClFN5O3S2
Anwendungsbeschreibung: PK11007 reactivates mutant p53 via selective alkylation of two cysteine residues without compromising DNA-binding ability.1 p53 target genes p21 and PUMA were activated by treatment with PK11007. Mutant p53-containing cancer cells were more sensitive to PK11007 than wild-type with mutant cells showing greatly reduced viability. It also generated high levels of reactive oxygen species and induced ER stress in a p53-independent (and dependent on glutathione depletion) manner that resulted in cell death. PK11007 inhibited cellular proliferation, induced apoptosis, and blocked cell migration in a panel of 17 breast cancer lines including triple-negative breast cancer (IC50s: 2.3 to 42.2 µM).2