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化學性質:
規格 | 10mM (in 1mL DMSO) 2mg 5mg |
CAS | 278603-08-0 |
別名 |
|
化學名 | 1-benzyl-3-hexadecyl-2-methylimidazol-1-ium;iodide |
分子式 | C27H45IN2 |
分子量 | 524.56 |
溶解度 | ≥ 25.9mg/mL in DMSO |
儲存條件 | Store at -20° C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
NH125 is a selective inhibitor of eEF-2 with IC50 value of 60 nM [1].
Eukaryotic elongation factor-2 kinase (eEF-2 kinase or eEF-2K), also known as calcium/calmodulin-dependent eukaryotic elongation factor 2 kinase (CaMKIII) is a highly conserved protein kinase in the calmodulin-mediated signaling pathway and plays an important role in regulating protein [1, 2].
NH125 is a potent eEF-2 inhibitor and has 1000- to >100000-fold more potent against eEF-2 compared with PKC, PKA and CamK-II. When tested with a panel of 10 cancer cell lines (C6, T98-G, U-138 MG, and so forth), NH125 treatment inhibited cell viability with IC50 value ranges from 0.7 to 4.8 μM. And NH125 decreased the cellular content of p-eEF-2 without affecting total content eEF-2 and arrested cell in G0-G1 phase in C6 glioma cells [1]. In HUVECs, NH125 treatment inhibited TNF-α-induced inflammatory responses at the dose of 1μM/L [3]. When tested with a panel of human cancer cell lines (glioblastoma, breast cancer, and so on), NH125 sensitized cells at the dose of 0.25 μM which thus reinforced the efficacy of ER stress-inducing drug by inhibiting eEF-2 [2].
In spontaneously hypertensive-SHR (10 wk old) rat model, administration of NH125 (500 μg·kg−1·day−1) for 6 weeks resulted in significant reduction SBP, reduced the increased expression of VCAM-1 and E-selectin and inhibited the increased ROS production and wall thickness in SHR [3].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278