PK11007

Catalog No.S8728

PK11007 Chemical Structure

Molecular Weight(MW): 236.63

PK11007 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR.

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Biological Activity

Description PK11007 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR.
Targets
p53 [1]
()
In vitro

PK11007 is a mild thiol alkylator with anticancer activity in several cell lines, especially those with mutationally compromised p53. It effectively kills cancer cells, especially with null or mutant p53 background, and shows only low cytotoxicity toward normal cells. PK11007 acts by two routes: p53 dependent and p53 independent. PK11007 stabilized p53 in vitro via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. Unstable p53 was reactivated by PK11007 in some cancer cell lines, leading to up-regulation of p53 target genes such as p21 and PUMA. PK11007 induces mainly caspase-independent cell death[1].

Protocol

Cell Research:

[1]

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  • Cell lines: p53 wild-type cell lines (WI-38, HUH-6, NUGC-4, SJSA-1) and p53 mutant cell lines (HUH-7, NUGC-3, SW480, MKN1)
  • Concentrations: 0-120 μM
  • Incubation Time: 24 h
  • Method:

    Cell viability assays


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 47 mg/mL (198.62 mM)
Water 47 mg/mL (198.62 mM)
Ethanol 23 mg/mL (97.19 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 236.63
Formula

C6H5ClN2O4S

CAS No. 38275-34-2
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID