1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. Rhosin hydrochloride

Rhosin hydrochloride 

Cat. No.: HY-12646 Purity: 99.93%
Handling Instructions

Rhosin hydrochloride 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 hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.

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

Rhosin hydrochloride Chemical Structure

Rhosin hydrochloride Chemical Structure

CAS No. : 1281870-42-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

Rhosin hydrochloride 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 hydrochloride induces cell apoptosis[1][2]. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3].

IC50 & Target

Kd: 0.4 uM (RhoA)[1]

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[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[3].
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[3].

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

394.86

Formula

C₂₀H₁₉ClN₆O

CAS No.

1281870-42-5

SMILES

O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[[email protected]](N)CC3=CNC4=C3C=CC=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (253.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5325 mL 12.6627 mL 25.3254 mL
5 mM 0.5065 mL 2.5325 mL 5.0651 mL
10 mM 0.2533 mL 1.2663 mL 2.5325 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.93%

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Keywords:

RhosinRasApoptosisMCF7cellsselectivestressresiliencyD1-MSNplasticityhyperexcitabilityInhibitorinhibitorinhibit

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Product Name:
Rhosin hydrochloride
Cat. No.:
HY-12646
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