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Description: Potent and selective polynucleotide kinase/phosphatase (PNKP) inhibitor
Chemical Name: 4a,7a-Dihydro-2-(1-hydroxyundecyl)-1-[(4-nitrophenyl)amino]-6-phenyl-1H-pyrrolo[3,4-b]pyridine-5,7(2H,6H)-dione
Purity: ≥98% (HPLC)

Biological Activity for A12B4C3

A12B4C3 is a potent and selective polynucleotide kinase/phosphatase (PNKP) inhibitor (IC50 = 60 nM). Displays no effect on calcineurin, protein PP-1 or APTX. Interrupts DNA repair and enhances radiosensitivity of human A549 lung carcinoma and MDA-MB-231 cells.

Compound Libraries for A12B4C3

A12B4C3 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for A12B4C3

M. Wt 534.65
Formula C30H38N4O5
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1005129-80-5
PubChem ID 6610064
Smiles O=C2N(C4=CC=CC=C4)C(C1C=CC(C(O)CCCCCCCCCC)N(NC3=CC=C([N+]([O-])=O)C=C3)C12)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for A12B4C3

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 53.47 100

Preparing Stock Solutions for A12B4C3

The following data is based on the product molecular weight 534.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.35 mL 18.7 mL
5 mM 0.37 mL 1.87 mL 3.74 mL
10 mM 0.19 mL 0.94 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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References for A12B4C3

References are publications that support the biological activity of the product.

Freschauf et al (2009) Identification of a small molecule inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase. Cancer Res. 69 7739 PMID: 19773431

Freschauf et al (2010) Mechanism of action of an imidopiperidine inhibitor of human polynucleotide kinase/phosphatase. J.Biol.Chem. 285 2351 PMID: 19940137

Schellenberg et al (2011) DNA end processing by polynucleotide kinase/phosphatase. Proc.Natl.Acad.Sci.U.S.A. 108 20855 PMID: 22184240

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Keywords: A12B4C3, A12B4C3 supplier, Potent, selective, polynucleotide, kinases, phosphatases, PKNP, inhibitors, inhibits, DNA, repair, Other, Kinases, 5097, Tocris Bioscience

Citations for A12B4C3

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