CAS NO: | 278603-08-0 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
2mg | 电议 |
5mg | 电议 |
Cas No. | 278603-08-0 |
化学名 | 1-benzyl-3-hexadecyl-2-methylimidazol-1-ium;iodide |
Canonical SMILES | CCCCCCCCCCCCCCCCN1C=C[N+](=C1C)CC2=CC=CC=C2.[I-] |
分子式 | C27H45IN2 |
分子量 | 524.56 |
溶解度 | ≥ 25.9mg/mL in DMSO |
储存条件 | 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 All other available size: ship with RT , or blue ice upon request |
产品描述 | 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]. It is also reported that NH125 inhibited protein kinase C (PKC), protein kinase A (PKA), and calmodulin-dependent kinase II (CamK-II) with IC50 value of 7.5 μM, 80 μM and >100 μM, respectively [1]. References: |