inhibitor of smooth muscle cell migration and proliferation, inhibits PKC signaling
CAS：193620-69-8
分子式：C23H19NO3
分子量：357.4
纯度：98%
存储：Store at -20°C

Background:

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

TAS-301 (1-10 μM) concentration-dependently inhibits PKC activation and Ca2+ influx, induced by PDGF, with 62.7% inhibition on PKC activation at 10 μM, and reduces PMA-induced AP-1, with 38% and 67.6% inhibition at 3 and 10 μM, respectively[1]. TAS-301 (0.3-3 μM) dose-dependently reduces the migration of cells induced by growth factors (PDGF-BB, IGF-1,HB-EGF). TAS-301 (1-10 μM) also decreases bFGF-induced BrdU incorporation, especially at 3 and 10 μM[2].

TAS-301 (3-100 mg/kg, p.o.) dose-dependently reduces the neointimal thickening and I/M ratio and decreases the level of intimal cells in rats 14 days after balloon injury[2].

Reference:
[1]. Muranaka Y, et al. TAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries. J Pharmacol Exp Ther. 1998 Jun;285(3):1280-6.
[2]. Sasaki E, et al. TAS-301 blocks receptor-operated calcium influx and inhibits rat vascular smooth muscle cell proliferation induced by basic fibroblast growth factor and platelet-derived growth factor. Jpn J Pharmacol. 2000 Nov;84(3):252-8.