PK11007 | Mutant p53 reactivator
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $240.00 |
PK11007 (874146-69-7) 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
References/Citations:
- Bauer et al. (2016), 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells; Proc. Natl. Acad. Sci. USA 113 E5271
- Synnott et al. (2018), Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007; Cancer Lett. 414 99
C15H11ClFN5O3S2
>98% HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
PK11007 (874146-69-7) 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
References/Citations:
- Bauer et al. (2016), 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells; Proc. Natl. Acad. Sci. USA 113 E5271
- Synnott et al. (2018), Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007; Cancer Lett. 414 99
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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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