Rhosin

Cat. No.: HY-12646A: FAQs
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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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Other In-stock Forms of Rhosin:

Rhosin hydrochloride

Other Forms of Rhosin:

Rhosin hydrochloride In-stock

24 Publications Citing Use of MCE Rhosin

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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

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

Rhosin Related Classifications

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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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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