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1281870-42-5

中文名称 1281870-42-5
英文名称 Rhosin (hydrochloride)
CAS 1281870-42-5
更新日期 2024/11/15 18:20:31
分子式 C20H19ClN6O
分子量 394.86
MOL 文件 1281870-42-5.mol
1281870-42-5 结构式 1281870-42-5 结构式

基本信息

中文别名
RHO抑制剂(RHOSIN盐酸盐)
英文别名
Rhosin HCl
G04 HYDROCHLORIDE
Rhosin (hydrochloride)
D-Tryptophan (2E)-2-(6-quinoxalinylmethylene)hydrazide hydrochloride
(R,E)-2-amino-3-(1H-indol-3-yl)-N'-(quinoxalin-6-ylmethylene)propanehydrazide hydrochloride

物理化学性质

储存条件-20°C储存
溶解度DMF: 10 mg/ml; DMSO: 5 mg/ml; Ethanol: 5 mg/ml; PBS (pH 7.2): insol
形态固体
颜色Light yellow to yellow

常见问题列表

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
TargetValue
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.
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