纯度:>98% by HPLC;NMR (Conforms)
分子式:C15H11ClFN5O3S2
分子量:427.85
溶剂:DMSO (>25 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):Reactivator of mutant p53
Function / Pharmacology: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