EC Number |
Inhibitors |
Structure |
---|
3.1.3.32 | 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione |
A12B4C3 |
|
3.1.3.32 | 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione |
i.e. A12B4C3, a potent, noncompetitive inhibitor of the phosphatase activity of human polynucleotide kinase/phosphatase in vitro. The inhibitor can form a ternary complex with PNKP and a DNA substrate, the inhibitor does not prevent DNA from binding to the phosphatase DNA binding site, but disrupts the secondary structure of PNKP, interaction between Trp402 of PNKP and the inhibitor. A12B4C3 sensitizes A549 human lung cancer cells to the topoisomerase I poison, camptothecin, but not the topoisomerase II poison, etoposide, in a manner similar to small interferingRNAagainst PNKP |
|
3.1.3.32 | 2-(hydroxy(3,4,5-trimethoxyphenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione |
A6B4C3 |
|
3.1.3.32 | 2-(hydroxy(phenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione |
A1B4C3 |
|
3.1.3.32 | 2-(hydroxy(thiophen-2-yl)methyl)-6-methyl-1-(phenylamino)-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione |
A39B1C2 |
|
3.1.3.32 | diphosphate |
no effect on 3'-phosphatase, inhibition of 5'-hydroxyl kinase |
|
3.1.3.32 | EDTA |
- |
|
3.1.3.32 | heparin |
- |
|
3.1.3.32 | heparin |
heparin exhibits an IC50 of 0.16 mg/ml |
|
3.1.3.32 | more |
optimization of a rapid high-throughput screening method for detection of DNA 3'-phosphatases and their inhibitors, overview |
|