| Name | 5-chloro-2-methylsulfonylpyrimidine-4-carboxylic acid |
|---|---|
| Synonyms |
2-methylsulfonyl-5-chloro-4-pyrimidine carboxylic acid
PK11000 2-methanesulfonyl-5-chloro-4-pyrimidinecarboxylic acid 2-methylsulfonyl-5-chloropyrimidine-4-carboxylic acid PK11000 ,S8728 5-chloro-2-methanesulfonyl-pyrimidine-4-carboxylic acid 5-chloro-2-(Methylsulfonyl)-4-pyriMidinecboxylic acid PK11000, 10 mM in DMSO PK-11000,HCC1143,MKN1,MCF10A,JimT1,mutant p53 cancer cells,BT549,HUH-7,NU-4,BT474,HCC1937,MCF7,SUM 159,PK11000,Inhibitor,MCF12A,DNA Alkylator/Crosslinker,SJSA-1,NU-3,MDM-2/p53,BT20,SW480,UACC812,inhibit,HUH-6,T47D,PK 11000,Hs578T(i8),SKBR3 PK-11000 4-carboxy-5-chloro-2-methylsulfonylpyrimidine 4-Pyrimidinecboxylic acid, 5-chloro-2-(methylsulfonyl) 2-methanesulfonyl-5-chloro-4-pyrimidinecboxylic acid PK 11000;PK-11000;PK |
| Description | PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53. |
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| Related Catalog | |
| 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]. |
| Cell Assay | 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]. |
| References |
| Molecular Formula | C6H5ClN2O4S |
|---|---|
| Molecular Weight | 236.63300 |
| Exact Mass | 235.96600 |
| PSA | 105.60000 |
| LogP | 1.31250 |
| Storage condition | -20℃ |
| HS Code | 2933599090 |
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| Precursor 1 | |
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| DownStream 1 | |
| HS Code | 2933599090 |
|---|---|
| Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |