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KRIBB11研究進(jìn)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/KRIBB11.htmlKRIBB11/a產(chǎn)品描述：KRIBB11 is an inhibitor of bHeat shock factor (HSF)
<a href="https://www.medchemexpress.com/KRIBB11.html">KRIBB11</a>產(chǎn)品描述：KRIBB11 is an inhibitor of <b>Heat shock factor (HSF)</b>, with <b>IC<sub>50</sub></b> of 1.2 μM.

IC50 & Target: IC50: 1.2 μM (HSF)

<i><b>In Vitro:</b></i> KRIBB11 blocks the induction of HSF1 downstream target proteins such as HSP27 and HSP70. KRIBB11 induces growth arrest and apoptosis of HCT-116 cells. KRIBB11 inhibits HSF1-dependent recruitment of p-TEFb (positive transcription elongation factor b) to the hsp70 promoter<sup>[1]</sup>. PARP and caspase-3 cleavage is increased in cells treated with KRIBB11. Incubating RKO with KRIBB11, shows a toxic threshold of about 10 µM, and an IC<sub>50</sub> of 20-30 µM<sup>[2]</sup>.

<i><b>In Vivo:</b></i> KRIBB11 (50 mg/kg, i.p.) results in a 47.4% inhibition of tumor growth in nude mice, without body weight loss<sup>[1]</sup>. <br><br>
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