货号 | 5393/50 |
别名 | 11-Cyclopentyl-2-[[2-ethoxy-4-[[4-( |
供应商 | Tocris |
生物活性 | Potent and selective ERK5 inhibitor; inhibits EGFR-induced ERK5 autophosphorylation (EC50 = 90 nM) and ERK5 enzymatic activity (IC50 = 162 nM). Exhibits at least 30-fold selectivity for ERK5 over LRRK2 in a cell based assay. Also selective for ERK5 over a panel of other kinases. Orally bioavailable. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 638.8 |
分子式 | C36H46N8O3 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
参考文献 | Denget al (2013) Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur.J.Med.Chem. 70 758. PMID: 24239623. Elkinset al (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J.Med.Chem. 56 4413. PMID: 23656407. |