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Veliparib (dihydrochloride)研究进

发布日期：2017-10-27   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/Veliparib-dihydrochloride.htmlVeliparib (dihydrochloride)/a产品描述：Veliparib (di
<a href="https://www.medchemexpress.com/Veliparib-dihydrochloride.html">Veliparib (dihydrochloride)</a>产品描述：Veliparib (dihydrochloride) is a potent inhibitor of <b>PARP1</b> and <b>PARP2</b> with <b>K<sub>i</sub></b> of 5.2 nM and 2.9 nM in cell-free assays, respectively.

IC50 & Target: Ki: 5.2 nM (PARP1), 2.9 nM (PARP2)

<i><b>In Vitro:</b></i> Veliparib is inactive to SIRT2 (>5 μM)<sup>[1]</sup>. Veliparib inhibits the PARP activity with EC<sub>50</sub> of 2 nM in C41 cells<sup>[2]</sup>. Veliparib can decrease the PAR levels in both irradiated and nonirradiated H460 cells. Veliparib reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. Veliparib increases apoptosis and autophagy in H460 cells when combination with radiation<sup>[3]</sup>. Veliparib inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. Veliparib (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. Veliparib shows effective radiosensitivity in oxic H1299 cells. Veliparib can attenuate the SF of hypoxic-irr<br><br>
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