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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA Repair Protein -A12B4C3
A12B4C3

Chemical Structure : A12B4C3

CAS No.: 1005129-80-5

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A12B4C3 (hPNKP inhibitor A12B4C3)

货号: 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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10 mg ￥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 534.657
分子式 C30H38N4O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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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