WF-536

WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

WF-536（1、3、10、30、100 μM）抑制 LLC 细胞的侵袭和迁移以及内皮细胞在 Matrigel 上的侵袭、迁移和毛细管样管的形成，在这两种细胞类型下均无细胞毒性或抗增殖作用[1]。 Cell Migration Assay [1] Cell Line: LLC cells, Human umbilical vein endothelial cells Concentration: 1, 3, 10, 30 μM Incubation Time: 6 h (tumor cells), 4 h (endothelial cells) Result: Significantly inhibited LLC-cell migration, with inhibitory rates of 23% and 44% at 10 and 30 μM, respectively. Cell Invasion Assay[1] Cell Line: LLC cells, Human umbilical vein endothelial cells Concentration: 1, 3, 10, 30 μM Incubation Time: 18 h Result: Showed significant and concentration-dependent inhibition of LLC-cell invasion. Cell Proliferation Assay[1] Cell Line: LLC cells, Human umbilical vein endothelial cells Concentration: 1, 30, 100 μM Incubation Time: 24, 48, 72, and 96 h Result: Showed no significant effect at 1-30 μM on the proliferation up to 96 h incubation, although the proliferation was decreased at 100 μM over 48 h.

WF-536（口服；0.3-3 mg/kg/天；持续 28 天）抑制小鼠 Lewis 肺癌 (LLC) 转移和 LLC 诱导的血管生成[1]。 Animal Model: C57BL/6 mice (male, 6-week old)[1] Dosage: 0.3, 1, 3 mg/kg Administration: Oral; daily; for 28 days Result: Significantly reduced the number of pulmonary metastatic colonies of LLC in a dose-dependent manner (0.3- 3 mg/kg).

[1]. Nakajima, Masahide et al. Wf-536 prevents tumor metastasis by inhibiting both tumor motility and angiogenic actions. European journal of pharmacology vol. 459,2-3 (2003): 113-20.