Locostatin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Locostatin 是一种有效且具有细胞渗透性的 Raf 激酶抑制剂蛋白 (RKIP)/Raf1 激酶相互作用抑制剂，也是细胞迁移的抑制剂。Locostatin 治疗导致丝裂原激活蛋白激酶 (MAPK) 信号通路（ERK 磷酸化）的激活，为我们的靶向协议提供强大的验证。

Locostatin is a potent and cell permeable inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.Locostatin treatment resulted in the activation of the mitogen-activated protein kinase (MAPK) signal pathway (ERK phosphorylation), providing a powerful validation of our targeting protocol.?Further, RKIP inhibition by locostatin reduces ECM components.?Moreover, the inhibition of RKIP by locostatin impaired cell proliferation and migration in both leiomyoma and myometrial cells.?Finally, locostatin treatment reduced GSK3β expression.?Therefore, even if the activation of MAPK pathway should increase proliferation and migration, the destabilization of GSK3β leads to the reduction of proliferation and migration of myometrial and leiomyoma cells.Compared to the CCl4 group, HYP (208.56 ± 6.12) μg/g, percentage of total collagen at overall region (1.91 ± 0.13), MMP-13/TIMP-1 (0.19 ± 0.01), MPO (1.45 ± 0.04) U/g, TGF-β (2652 ± 91.20), PDGF-AA (3897 ± 290.69), and E-selectin (1569 ± 66.48) in the liver tissues were decreased significantly in the locostatin-treated group.

——

——

——

MAPK/ERK Signaling

Raf

Raf-1

——

——

133812-16-5

245.27

C14H15NO3

>98% (HPLC)

ethanol:10 mg/ml;DMSO:5 mg/ml;DMF:5 mg/ml

CC=CC(=O)N1C(COC1=O)CC2=CC=CC=C2

——

(-20℃)

With Ice Pack

≥ 2 years