NH-125

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的真核 eEF-2 激酶 (eEF2K) 抑制剂，体外 IC50 为 60 nM，可阻断完整细胞中 eEF-2 的磷酸化。

A potent eukaryotic eEF-2 kinase (eEF2K) inhibitor with IC50 of 60 nM in vitro and blocks the phosphorylation of eEF-2 in intact cells; shows relative selectivity over other protein kinases: PKC (IC50=7.5 uM), PKA (IC(50=80 uM), and CaMKII (IC50>100 uM); shows efficacious anti-proliferation activityt against different cancer cells.

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. Anticancer effect of NH125 is not mediated through inhibition of eEF2K. Inhibition of cell growth correlates with induction of peEF2.

——

NH 125 | NH125

Nuclear Receptor/Transcription Factor

eIF

CaMKII|eEF-2kinase|PKA|PKC

Cancer

——

278603-08-0

524.56

C27H45IN2

>98% (HPLC)

DMSO: 52.5 mg/mL (100 mM); Ethanol: 39.3 mg/mL (75 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CC1=[N+](CC2=CC=CC=C2)C=CN1CCCCCCCCCCCCCCCC.[I-]

1H-Imidazolium, 1-hexadecyl-2-methyl-3-(phenylmethyl)-, iodide (9CI)

(-20℃)

With Ice Pack

≥ 2 years