1005129-80-5

1005129-80-5 structure

Name: A12B4C3
Chemical Name: 2-(1-hydroxyundecyl)-1-(4-nitroanilino)-6-phenyl-4a,7a-dihydro-2H-pyrrolo[3,4-b]pyridine-5,7-dione
CAS Number: 1005129-80-5
Molecular Formula: C₃₀H₃₈N₄O₅
Molecular Weight: 534.64700
Catalog: Research Areas Cancer
Create Date: 2016-09-24 14:03:25
Modify Date: 2024-01-11 00:17:26
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells[1].

Name	2-(1-hydroxyundecyl)-1-(4-nitroanilino)-6-phenyl-4a,7a-dihydro-2H-pyrrolo[3,4-b]pyridine-5,7-dione
Synonyms	4a,7a-Dihydro-2-(1-hydroxyundecyl)-1-[(4-nitrophenyl)amino]-6-phenyl-1H-pyrrolo[3,4-b]pyridine-5,7(2H,6H)-dione 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7-(2H,4aH)dione A12B4C3

Description	A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
Target	IC50: 0.06 μM (hPNKP)[1]
In Vitro	A12B4C3 (0-10 μM) strongly inhibits hPNKP phosphatase activity[1]. A12B4C3 (0-100 μM; 72 h) reduces A549 and MDA-MB-231 cell proliferation in a dose dependent manner[1]. A12B4C3 (1 μM; 24 h) increases the radiosensitivity of A549 cells[1]. Cell Proliferation Assay[1] 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[1] 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.
References	[1]. Freschauf GK, et al. Identification of a small molecule inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase. Cancer Res. 2009 Oct 1;69(19):7739-46.