Rhosin

Cat. No.: HY-12646A Purity: 95.08%: Data Sheet
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Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d 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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Rhosin hydrochloride) usually boasts enhanced water solubility and stability.

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

Rhosin Chemical Structure

CAS No. : 1173671-63-0

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Rhosin:

Rhosin hydrochloride

Other Forms of Rhosin:

Rhosin hydrochloride In-stock

29 Publications Citing Use of MCE Rhosin

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Biological Activity
Purity & Documentation
References
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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 K_d 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].

MedChemExpress (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].

MedChemExpress (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

CAS No.

1173671-63-0

Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4

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 : 50 mg/mL (139.51 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7902 mL	13.9509 mL	27.9018 mL
5 mM	0.5580 mL	2.7902 mL	5.5804 mL
10 mM	0.2790 mL	1.3951 mL	2.7902 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 95.08%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (247 KB) HNMR (271 KB) RP-HPLC (250 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

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

[2]. 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. [Content Brief]

[3]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7902 mL	13.9509 mL	27.9018 mL	69.7545 mL
	5 mM	0.5580 mL	2.7902 mL	5.5804 mL	13.9509 mL
	10 mM	0.2790 mL	1.3951 mL	2.7902 mL	6.9754 mL
	15 mM	0.1860 mL	0.9301 mL	1.8601 mL	4.6503 mL
	20 mM	0.1395 mL	0.6975 mL	1.3951 mL	3.4877 mL
	25 mM	0.1116 mL	0.5580 mL	1.1161 mL	2.7902 mL
	30 mM	0.0930 mL	0.4650 mL	0.9301 mL	2.3251 mL
	40 mM	0.0698 mL	0.3488 mL	0.6975 mL	1.7439 mL
	50 mM	0.0558 mL	0.2790 mL	0.5580 mL	1.3951 mL
	60 mM	0.0465 mL	0.2325 mL	0.4650 mL	1.1626 mL
	80 mM	0.0349 mL	0.1744 mL	0.3488 mL	0.8719 mL
	100 mM	0.0279 mL	0.1395 mL	0.2790 mL	0.6975 mL

Rhosin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rhosin1173671-63-0RasApoptosisMCF7cellsselectivestressresiliencyD1-MSNplasticityhyperexcitabilityInhibitorinhibitorinhibit

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