产品说明书

Rhosin HCl

Print
Chemical Structure| 1281870-42-5 同义名 : Rhosin (hydrochloride);Rhosin hydrochloride;G04;G04 hydrochloride
CAS号 : 1281870-42-5
货号 : A708952
分子式 : C20H19ClN6O
纯度 : 99%+
分子量 : 394.858
MDL号 : MFCD18794648
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(126.63 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 15 mg/mL(37.99 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 RhoA is a ubiquitously expressed cytoplasmic protein that belongs to the family of small GTPases. RhoA acts as a molecular switch that is activated in response to binding of chemokines, cytokines, and growth factors, and via mDia and the ROCK signaling cascade regulates the activation of cytoskeletal proteins, and other factors[3].Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis[4]. In cells, Rhosin specifically inhibited RhoA activity and RhoA-mediated cellular function without affecting Cdc42 or Rac1 signaling activities. By suppressing RhoA or RhoC activity, Rhosin could inhibit mammary sphere formation by breast cancer cells, suppress invasion of mammary epithelial cells, and induce neurite outgrowth of PC12 cells in synergy with NGF. Rhosin HCL dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells[5]. Rhosin HCL promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability. Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells. 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[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.66mL

2.53mL

1.27mL

25.33mL

5.07mL

2.53mL

参考文献

[1]Shang X, Marchioni F, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60.

[2]Shang X, Marchioni F, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710.

[3] Matthias Bros,et al. RhoA as a Key Regulator of Innate and Adaptive Immunity. Cells. 2019 Jul 17;8(7):733.

[4] Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60.

[5] Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710.

[6]Francis TC, et al. The Selective RhoA Inhibitor Rhosin Promotes Stress Resiliency Through Enhancing D1-Medium Spiny Neuron Plasticity and Reducing Hyperexcitability. Biol Psychiatry. 2019;85(12):1001-1010.