英文名称:
Rhosin (hydrochloride)
英文同义词:
Rhosin (hydrochloride);Rhosin HCl;(R,E)-2-amino-3-(1H-indol-3-yl)-N-(quinoxalin-6-ylmethylene)propanehydrazide hydrochloride;D-Tryptophan (2E)-2-(6-quinoxalinylmethylene)hydrazide hydrochloride;G04 HYDROCHLORIDE
生物活性
Rhosin (G04) hydrochloride (HCl) 是RhoA亚家族 Rho GTPases 的强效特异性抑制剂，Kd值约为0.4 uM。Rhosin hydrochloride 可诱导细胞凋亡。
靶点
Target Value
Rho
(Cell-free assay) 0.4 μM(Kd)
Rho
(Cell-free assay)
0.4 μM(Kd)
体外研究
Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC 50 ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells.
体内研究
Rhosin (40 mg/kg; i.p.) treatment prevents social avoidance caused by social defeat stress. Rhosin also blocks sucrose preference deficits induced by defeat in C57Bl6/J (Jackson) mice.
Rhosin (30 µM; bilateral, intra- Nucleus Accumbens (NAc) infusions) attenuates stress-induced social avoidance. Rhosin blocks stress-induced hyperexcitability in NAc dopamine 1 receptor medium spiny neurons (D1-MSNs). Rhosin prevents decreased excitatory transmission on NAc D1-MSNs. Rhosin enhances spine density in defeat mice.
Animal Model: D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background
Dosage: 40 mg/kg
Administration: I.p.
Result: Rhosin was systemically administered 15 min prior to defeat to block RhoA activation. While defeat significantly reduced the time that experimental mice spent interacting with a novel mouse, Rhosin administration suppressed this effect without affecting locomotor behaviors.
Animal Model:
D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background
Result:
Rhosin was systemically administered 15 min prior to defeat to block RhoA activation. While defeat significantly reduced the time that experimental mice spent interacting with a novel mouse, Rhosin administration suppressed this effect without affecting locomotor behaviors.
