A stabilizer of mutant p53
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PK11000

Item No. 37306

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-chloro-2-(methylsulfonyl)-4-pyrimidinecarboxylic acid
CAS Number
38275-34-2
Molecular Formula
C6H5ClN2O4S
Formula Weight
236.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
225 nm
SMILES
O=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O
InChi Code
InChI=1S/C6H5ClN2O4S/c1-14(12,13)6-8-2-3(7)4(9-6)5(10)11/h2H,1H3,(H,10,11)
InChi Key
WZUPWJVRWIVWEF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 mg

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    500 mg

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    Product Description

    PK11000 is a stabilizer of mutant p53.1 It covalently binds to Cys182 and Cys277, increases the thermal stability, and inhibits the aggregation of the p53Y220C DNA-binding domain when used at a concentration of 1 mM. PK11000 selectively decreases the viability of mutant p53-expressing SW480 (p53R273H,P309S), NUGC-3 and Huh7 (p53Y220C), and MKN1 (p53V143A) cancer cells over wild-type p53-expressing NUGC-4, HuH-6, and SJSA-1 cancer cells. However, it is not selective between H1299 p53-/- and H1299 p53R175H non-small cell lung cancer (NSCLC) cells. PK11000 (15 µM) increases the expression of the p53 target genes p21 and PUMA and decreases the expression of the p53 target gene MDM2 in Huh7 and MKN1 cells. It also increases the levels of reactive oxygen species (ROS) in Huh7 and MKN1 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bauer, M.R., Joerger, A.C., and Fersht, A.R. 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells. Proc. Natl. Acad. Sci. U S A 113(36), E5271-E5280 (2016).