Rhosin hydrochloride

SKU: orb1218965

Description

Rhosin hydrochloride is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin hydrochloride does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride causes cell apoptosis.

Key Properties

• CAS Number: 1281870-42-5
• MW: 394.86
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₉ClN₆O
• SMILES: O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4.Cl
• Target: Apoptosis
• Solubility: DMSO:100 mg/mL (253.25 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Apoptosis