CAS NO: | 278603-08-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase(eEF-2K/CaMKIII), also can induce eEF2 phosphorylation, with anIC50of 60 nM for eEF-2K[1][2]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | NH125 inhibits eEF-2 kinase activity (IC50= 60 nM) in vitro, blocks the phosphorylation of eEF-2 in intact cells, and shows relative selectivity over other protein kinases: protein kinase C (IC50= 7.5 μM), protein kinase A (IC50= 80 μM), and calmodulin-dependent kinase II (IC50>100 μM). NH125 decreases the viability of 10 cancer cell lines with IC50s ranging from 0.7 to 4.7 μM. Forced overexpression of eEF-2 kinase in a glioma cell line produces 10-fold resistance to NH125. In conclusion, these results suggest that identification of potent inhibitors of eEF-2 kinase may lead to the development of new types of anticancer drugs[1]. Anticancer effect of NH125 is not mediated through inhibition of eEF2K. Inhibition of cell growth correlates with induction of peEF2[2]. | ||||||||||||||||
分子量 | 524.56 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H45IN2 | ||||||||||||||||
CAS 号 | 278603-08-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 50 mg/mL(95.32 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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