生物活性 | |||
---|---|---|---|
描述 | SecinH3 is a selective cytohesin inhibitor for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7 with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM respectively. SecinH3 almost completely blocks the insulin-dependent transcriptional repression of IGFBP1 with an IC50 of 2.2 μM. Insulin-stimulated translocation of ARF6 to the plasma membrane is also inhibited by SecinH3. SecinH3-treated mice show increased expression of gluconeogenic genes, reduced expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduced liver glycogen stores, and a compensatory increase in plasma insulin[3]. SecinH3, a cytohesin inhibitor, has neuroprotective effects against mutant SOD1 toxicity. SecinH3 was demonstrated to successfully attenuate the TDP-43 (transactivating response region DNA binding protein 43) Q331K-induced neuronal toxicity by suppressing ER (endoplasmic reticulum) stress-mediated apoptosis and enhancing the autophagic flux[4]. SecinH3 can significantly inhibit the cytohesins and then relieve the lung injury induced by the sepsis of rats[5]. Treating mice bearing H460 xenografts with SecinH3 showed the antiproliferative and pro-apoptotic effect of SecinH3 in vivo[6]. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.86mL 2.17mL 1.09mL |
21.72mL 4.34mL 2.17mL |
参考文献 |
---|