PK11007, Reactivator of mutant p53 (TBI4176)

Description

Product Details

Formal Name: 5-Chloro-2-[(4-fluorophenyl)methylsulfonyl]-N-(5-methyl-1,3,4-thiadiazol-2-yl)pyrimidine-4-carboxamide

Molecular Formula: C₁₅H₁₁ClFN₅O₃S₂

Formula Weight: 427.8

CAS Number: 874146-69-7

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Reactivator of mutant p53

Functions

Reactivates mutant p53 via selective alkylation of two cysteine residues without compromising DNA-binding ability. 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. 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).

Application Procedures

First dissolved in DMSO (> 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4176_PK11007_datasheet

MSDS:

TBI4176_PK11007_MSDS

Research use only.