1281870-42-5

中文名称:

1281870-42-5

中文同义词:

RHO抑制剂(RHOSIN盐酸盐)

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

CAS号:

1281870-42-5

分子式:

分子量:

0

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

Mol File

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)

Target

Value

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

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.