SLx-2119

"目录号: HY-15307

Cell Cycle/DNA DamageTGF-beta/SmadStem Cell/Wnt-

SLx-2119 是一种有效的ROCK2抑制剂，IC50值为 105 nM，选择性是 ROCK1 的 200 多倍，对 ROCK1 的IC50值为 24 μM。

ROCK

相关产品

Y-27632 dihydrochloride-Y-33075 dihydrochloride-Narciclasine-GSK269962A-Fasudil Hydrochloride-GSK429286A-LX7101-ROCK inhibitor-Thiazovivin-SR-3677-K-115-RKI-1447-chroman 1-H-1152 dihydrochloride-AR-13324 hydrochloride-

生物活性

Description

SLx-2119 is a selective inhibitor ofROCK2withIC50of 105 nM, more than 200 fold selecivity over ROCK1 (IC50=24 μM).

IC50& Target

IC50: 105 nM (ROCK2)

In Vitro

SLx-2119 (40 μM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with SLx-2119, shows a 5-times higher background than the other arrays[1].

In Vivo

KD025 (100, 200 or 300?mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. KD025 is at least as efficacious in aged, diabetic or female mice, as in normal adult males[2].

References

[1].Boerma, M., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul Fibrinolysis, 2008. 19(7): p. 709-18.

[2].Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol, 2014. 1(1): p. 2-14.