A12B4C3 |CAS:1005129-80-5 Probechem Biochemicals

Chemical Structure : A12B4C3

A12B4C3 (hPNKP inhibitor A12B4C3)

Catalog No.: PC-35266Not For Human Use, Lab Use Only.

A12B4C3 is a potent, specific human polynucleotide kinase/phosphatase (hPNKP) inhibitor, inhibits hPNKP phosphatase activity with IC50 of 60 nM.

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Biological Activity

A12B4C3 is a potent, specific human polynucleotide kinase/phosphatase (hPNKP) inhibitor, inhibits hPNKP phosphatase activity with IC50 of 60 nM.

A12B4C3 displayed no inhibition of two well-known eukaryotic protein phosphatases, calcineurin and protein phosphatase-1, or APTX, another human DNA 3'-phosphatase.

A12B4C3 enhanced the radiosensitivity of human A549 lung carcinoma and MDA-MB-231 breast adenocarcinoma cells, which was almost identical to the increased sensitivity resulting from shRNA-mediated depletion of hPNKP.

A12B4C3 sensitizes A549 human lung cancer cells to the topoisomerase I poison, camptothecin, but not the topoisomerase II poison, etoposide.

A12B4C3 also inhibits the repair of DNA single and double strand breaks following exposure of cells to ionizing radiation, but does not inhibit two other key strand-break repair enzymes, DNA polymerase beta or DNA ligase III.

Physicochemical Properties

M.Wt	534.657
Formula	C30H38N4O5
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4a,7a-Dihydro-2-(1-hydroxyundecyl)-1-[(4-nitrophenyl)amino]-6-phenyl-1H-pyrrolo[3,4-b]pyridine-5,7(2H,6H)-dione

References

1. Freschauf GK, et al. Cancer Res. 2009 Oct 1;69(19):7739-46.

2. Freschauf GK, et al. J Biol Chem. 2010 Jan 22;285(4):2351-60.

3. Zereshkian A, et al. Nucl Med Biol. 2014 May-Jun;41(5):377-83.

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A12B4C3 (hPNKP inhibitor A12B4C3)

Biological Activity

Physicochemical Properties

References

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