| 货号 | 4132/50 |
| 别名 | 2-[[2-Ethoxy-4-(4-hydroxy-1-piperid |
| 供应商 | Tocris |
| 生物活性 | ERK5 (BMK1) and BRD4 inhibitor (Kd values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kd values are 190, 600 and 890 nM). Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. Also reduces BMK1-dependent transactivating activity of MEF2C. Inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 474.55 |
| 分子式 | C26H30N6O3 |
| 可溶性/溶解性 | Soluble to 40 mM in DMSO |
| 参考文献 | Linet al (2016) ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 113 11865. PMID: 27679845. Erazoet al (2013) Canonical and kinase activity-independent mechanisms for extracellular signal-regulated kinase 5 (ERK5) nuclear translocation require dissociation of Hsp90 from the ERK5-Cdc37 complex. Mol.Cell Biol. 33 1671. PMID: 23428871. Denget al (2011) Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a potent and selective inhibitor of big MAP kinase 1. ACS Med.Chem.Lett. 2 195. PMID: 21412406. Yang and Lee (2011) Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin.Cancer Res. 17 3527. PMID: 21385929. Yanget al (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 18 258. PMID: 20832753. |