NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, also a potent histidine kinase inhibitor.
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产品名称 | CaMKII ↓ ↑ | CaMKIII ↓ ↑ | CaMKKα ↓ ↑ | CaMKKβ ↓ ↑ | PKD ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
KN-62 |
+
CaMKII, Ki: 0.9 μM |
98% | |||||||||||||||||
KN-93 |
++
CaMKII, Ki: 0.37 μM |
98% | |||||||||||||||||
NH125 |
+++
eEF-2 kinase, IC50: 60 nM |
99%+ | |||||||||||||||||
STO-609 |
++
CaM-KKα, Ki: 0.25 μM |
++++
CaM-KKβ, Ki: 47 nM |
98% | ||||||||||||||||
CID755673 |
+++
PKD2, IC50: 227 nM PKD1, IC50: 180 nM |
99%+ | |||||||||||||||||
CRT0066101 2HCl |
++++
PKD2, IC50: 2 nM PKD1, IC50: 1 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | H125 is a selective eEF2K inhibitor with IC50 value of 60nM in vitro. It blocked the phosphorylation of eEF-2 in intact C6 glioma cells at 1μM post 12h. It decreased the viability of 10 cancer cell lines from rat glioblastoma, human glioblastoma, human ovarian carcinoma, human cervical carcinoma, human prostate carcinoma, human ovarian carcinoma and human breast carcinoma with IC50 values ranging from 0.7 to 4.7μM[3]. On the contrary, some study showed that NH125 was more correlated with induction of eEF2 phosphorylation than inhibition of eEF2K[4]. |
Dose | Mice: 1 mg/kg[3] (i.p.); 25 mg/kg[4] (i.v.) |
Administration | i.p., i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.91mL 0.38mL 0.19mL |
9.53mL 1.91mL 0.95mL |
19.06mL 3.81mL 1.91mL |
CAS号 | 278603-08-0 |
分子式 | C27H45IN2 |
分子量 | 524.564 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 50 mg/mL(95.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |