2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. Rhosin

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.

CAS No. : 1173671-63-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 40 publication(s) in Google Scholar

Other Forms of Rhosin:

Rhosin Related Antibodies

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Rhosin

ELISA
RT-PCR
WB

    Rhosin purchased from MedChemExpress. Usage Cited in: Nature. 2025 Sep;645(8079):244-253.  [Abstract]

    Rhosin hydrochloride (Rhosin) (50 μM; 5 min) inhibited RhoA activity and diminished cGMP-stimulated ROCK and MLC phosphorylation in mature BMDCs.

    Rhosin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 22;16(1):2821.  [Abstract]

    The RhoA inhibitor Rhosin hydrochloride (40 μM) significantly reduced the increased expression of p-MLC, α-SMA, and COL-I induced by Sema4D treatment.

    Rhosin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Mar 14;14(1):1402.  [Abstract]

    Rhosin hydrochloride (Rhosin) (30 µM) blocked the increase in the activated forms of PDGF-AA in the PCK1-KO MIHA cell supernatant.

    Rhosin purchased from MedChemExpress. Usage Cited in: Circulation. 2021 May 4;143(18):1775-1792.  [Abstract]

    RhoA inhibitor Rhosin hydrochloride (Rhosin) (30 μg/100 g; respiratory tract injection; 14 d) efficiently blocked the rescue effects of GGPP after statin treatment on hypoxia-enhanced CaSR and HIMF gene expression in pulmonary arteries of rats.

    Rhosin purchased from MedChemExpress. Usage Cited in: Circulation. 2021 May 4;143(18):1775-1792.  [Abstract]

    Western blot analysis of hypoxia-altered ROCK2 phosphorylation and the effects of Rhosin hydrochloride (Rhosin) (30 μg/100 g; respiratory tract injection; 14 d) in pulmonary arteries of rats exposed to normoxia or hypoxia.

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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].

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

    Rhosin Related Antibodies
    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.
    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; Need ultrasonic; 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
    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.74%

    SDS (393 KB)

    COA (247 KB) HNMR (488 KB) RP-HPLC (257 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References

    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.

    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
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    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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