A12B4C3

Research use only, not for human use.

A12B4C3 (hPNKP inhibitor A12B4C3) is a specific, noncompetitive inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase (hPNKP) with C50 of 60 nM.

A12B4C3 (hPNKP inhibitor A12B4C3) is a specific, noncompetitive inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase (hPNKP) with C50 of 60 nM, displays no inhibition of calcineurin and protein phosphatase-1 or APTX; A12B4C3 enhanced the radiosensitivity of human A549 lung carcinoma and MDA-MB-231 breast adenocarcinoma cells, failed to increase the radiosensitivity of the hPNKP-depleted cells; 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.

A12B4C3 (0-10 μM) strongly inhibits hPNKP phosphatase activity.A12B4C3 (0-100 μM; 72 h) reduces A549 and MDA-MB-231 cell proliferation in a dose dependent manner.A12B4C3 (1 μM; 24 h) increases the radiosensitivity of A549 cells. Cell Proliferation Assay Cell Line:A549 and MDA-MB-231 Concentration:0, 1, 5, 10, 50 and 100 μM Incubation Time:72 h Result:Reduced cell proliferation in a dose dependent manner, and up to ~50% at 100 μM.Cell Proliferation Assay Cell Line:A549 and MDA-MB-231 (incubated with A12B4C3 for 2h then irradiated 0-10 Gy)Concentration:1 μM Incubation Time:24 h Result:Almost doubled the radiosensitivity of A549 cells.

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hPNKP inhibitor A12B4C3

Cell Cycle/DNA Damage

DNA Repair Protein

DNA Repair Protein

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1005129-80-5

534.657

C30H38N4O5

>98% (HPLC)

In Vitro:?DMSO : 53 mg/mL (99.13 mM)

O=C1N(C2=CC=CC=C2)C(C3C1C=CC(C(O)CCCCCCCCCC)N3NC4=CC=C([N+]([O-])=O)C=C4)=O

4a,7a-Dihydro-2-(1-hydroxyundecyl)-1-[(4-nitrophenyl)amino]-6-phenyl-1H-pyrrolo[3,4-b]pyridine-5,7(2H,6H)-dione

(-20℃)

With Ice Pack

≥ 2 years