1. Apoptosis
  2. MDM-2/p53

PK11007 

Cat. No.: HY-U00447 Purity: 99.74%
Handling Instructions

PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

For research use only. We do not sell to patients.

PK11007 Chemical Structure

PK11007 Chemical Structure

CAS No. : 38275-34-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
25 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

IC50 & Target

p53[1]

In Vitro

PK11007 (15-30 µM) reduces the viability of mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S). PK11007 also shows inhibitory activities against the p53 wt cancer cell lines HUH-6 and NUGC-4, as well as the fibroblast cell line WI-38 only at high concentrations (60 and 120 µM). PK11007 increases levels of p53 target genes and activates the unfolded protein response pathway. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells. PK11007 induces cell death via caspase-independent pathways. PK11007 (30, 60 µM) induces reactive oxygen species (ROS) especially in mutant p53 cells[1]. PK11007 inhibits the proliferation of a panel of 17 breast cell lines, with IC50s ranging from 2.3 to 42.2 μM[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (422.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2260 mL 21.1300 mL 42.2601 mL
5 mM 0.8452 mL 4.2260 mL 8.4520 mL
10 mM 0.4226 mL 2.1130 mL 4.2260 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cell viability is measured using the CellTiter-Fluor cell viability assay kit. Cells are seeded in 96-well plates at 7,500-15,000 cells per well and incubated overnight. Samples are prepared in medium with a twice-as-high compound (including PK11007), and DMSO concentration then added to an equivalent volume of growth medium, yielding a final DMSO concentration of 0.5%. After incubating of cells for 23 h or the respective time period, CellTiter-Fluor reagent is added to each well and incubated again for 45 min. Fluorescence is then recorded on a PHERAstar plate reader using 400/500 nm excitation/emission filters. Experiments are performed in quadruplicate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

236.63

Formula

C₆H₅ClN₂O₄S

CAS No.

38275-34-2

SMILES

O=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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PK11007
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PK11007

Cat. No.: HY-U00447