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CCT251236研究進展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/CCT251236.htmlCCT251236/a產(chǎn)品描述：CCT251236 is an orally available pirin ligand f
<a href="https://www.medchemexpress.com/CCT251236.html">CCT251236</a>產(chǎn)品描述：CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an <b>IC<sub>50</sub></b> of 19 nM for inhibition of HSF1-mediated <b>HSP72</b> induction.

IC50 & Target: IC50: 19 nM (HSF1-mediated HSP72 induction)<sup>[1]</sup>

<i><b>In Vitro:</b></i> CCT251236 displays the desired balance of <i>in vitro</i> properties, while maintaining excellent cellular activity with an IC<sub>50</sub> of 19 nM. The free GI<sub>50</sub> in SK-OV-3 cells is 1.1 nM. Western blotting confirms that CCT251236 blocks the HSF1-mediated induction of both HSP72 and HSP27 as representative heat shock proteins, following treatment with the HSP90 inhibitor 17AAG. Also, qPCR analysis demonstrates that CCT251236 inhibits the induction of HSP72 at the mRNA level, clearly blocking the induction of HSPA1A gene expression with an IC<sub>50</sub> of 40 nM<sup>[1]</sup>.



<i><b>In Vivo:</b></i> CCT251236 possesses low total blood clearance (10% hepatic blood fl<br><br>
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