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DC10851  (CAS:38275-34-2)
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PK11007 is a thiol-reactive anticancer agent that stabilizes wild type and mutant p53 through selective alkylation of two surface cysteines without interfering with its DNA binding.
CAS Number: 38275-34-2


Molecular Weight: 236.6
Molecular Formula: C6H5ClN2O4S
Quality Control: HPLCNMR LC/MS(Please contact us to get the QC report)
Synonyms: PK 11007PK-11007PK11007
Chemical Name: 5-Chloro-2-(methylsulfonyl)-4-pyrimidinecarboxylic acid
Storage: 2 years -20C Powder, 2 weeks4C in DMSO,6 months-80C in DMSO
Note: Products for research use only, not for human use
PK11007 was able to increase the thermal stability of p53. This compound was then tested on p53 wild type, mutant, and knockout cancer cell lines to determine its effect both dependent and independent of a functional p53 protein. PK11007 reduced the viability of each of these cell lines, with those containing a mutant p53 protein demonstrating the largest reduction in viability. This data demonstrated that although this compound is able to work through p53, this was not the sole mechanism involved. Because of this, various other mechanisms of action involved in cell death were tested. First, p53 target genes were assessed and found to be upregulated upon drug exposure, demonstrating partial restoration in the function of mutant p53 proteins. In addition, PK11007 upregulated proteins involved in the unfolded protein response (UPR) pathway, a cell stress response that inhibits the production of misfolded proteins. PK11007 also increased the levels of reactive oxygen species (ROS), compounds known to kill cancer cells and directly increase p53 levels.PK11007 was found to be an efficacious drug on cancer cells both with and without p53 mutations, showing its broad potential efficacy for various cancers. Although animal studies will need to be performed before clinical trials can be implemented, these new compounds have the potential to become therapeutic agents for a variety of cancers.
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