生物活性 | |||
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描述 | LIMK1 and LIMK2 regulate the actin cytoskeleton by phosphorylating and inactivating the cofilin family of actin-depolymerizing factors; LIMK1 also acts to destabilize microtubules and regulates cell motility, including tumor metastasis. The initial lead compound BMS-3 is a potent inhibitor of both LIMK activity and tubulin polymerization. In A549 cells, BMS-3 caused a dose-dependent reduction in cell count and induced mitotic arrest as shown by increases in total nuclear DNA intensity and histone H3 phosphorylation after 24 h treatment. The Affymetrix array contains probesets for 17 tubulin subunits; a dose-related decrease in signal for up to eight of these was seen with the treatment of BMS-3 suggesting it reduced the levels of tubulin transcripts. Relative to the vehicle control, addition of 10 μmol/L BMS-3 also decreased the rate and level of microtubule polymerization [2]. Inhibition of LIMK1 by BMS-3 resulted in lower levels of actin polymerization during capacitation and a dramatic decrease in the percentage of sperm that undergo acrosomal exocytosis [1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.65mL 2.33mL 1.16mL |
23.30mL 4.66mL 2.33mL |
参考文献 |
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