1. GPCR/G Protein
    Apoptosis
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    Apoptosis
  3. Rhosin

Rhosin 

Cat. No.: HY-12646A
Handling Instructions

Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which 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 induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.

For research use only. We do not sell to patients.

Rhosin Chemical Structure

Rhosin Chemical Structure

CAS No. : 1173671-63-0

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Description

Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which 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 induces cell apoptosis[1][2]. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3].

IC50 & Target

Kd: 0.4 uM (RhoA)[1]

In Vitro

Rhosin 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background[3]
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.
Molecular Weight

358.40

Formula

C₂₀H₁₈N₆O

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Rhosin
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