1311143-71-1
1311143-71-1 結(jié)構(gòu)式
基本信息
英文別名
JH295N-[(3Z)-3-[(2-Ethyl-4-methyl-1H-imidazol-5-yl)methylene]-2,3-dihydro-2-oxo-1H-indol-5-yl]-2-propynamide
物理化學(xué)性質(zhì)
密度1.375±0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at -20°C,unstable in solution, ready to use.
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)10?+-.0.20(Predicted)
形態(tài)Solid
顏色Yellow to orange
常見問題列表
生物活性
JH295 是一種有效，不可逆和選擇性的 NIMA-related kinase 2 (Nek2) 抑制劑，IC50 為 770 nM。JH295 通過 Cys22 的烷基化抑制細(xì)胞 Nek2。JH295 對(duì)有絲分裂激酶 Cdk1，Aurora B 或 Plk1 沒有活性，并且不會(huì)干擾雙極紡錘體組件或紡錘體組件檢查點(diǎn)。靶點(diǎn)
IC50: 770 nM (Nek2)
體外研究
JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC 50 of ~1.3 μM, whereas it has little effect on the C22V mutant.
Western Blot Analysis
| Cell Line: | RPMI7951 cells |
| Concentration: | 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM |
| Incubation Time: | 45 minutes |
| Result: | Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant. |