Rhosin
Based on 39 publication(s) in Google Scholar
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.
- Purity: 98.74%
- CAS No.: 1173671-63-0
- Formula: C20H18N6O
- Molecular Weight:358.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Rhosin
More- Nature. 2025 Sep;645(8079):244-253. [Abstract]
- Circulation. 2021 May 4;143(18):1775-1792. [Abstract]
- Cancer Res. 2022 Feb 15;82(4):681-694. [Abstract]
- Nat Commun. 2025 Mar 22;16(1):2821. [Abstract]
- Nat Commun. 2023 Mar 14;14(1):1402. [Abstract]
- Exp Mol Med. 2025 May;57(5):1064-1077. [Abstract]
- Neuron. 2025 Nov 26:S0896-6273(25)00842-6. [Abstract]
- Redox Biol. 2025 May:82:103596. [Abstract]
- Theranostics. 2022 May 9;12(8):3847-3861. [Abstract]
- J Clin Invest. 2025 Jun 2;135(11):e184158. [Abstract]
- Cell Death Dis. 2026 Mar 18;17(1):281. [Abstract]
- Cell Death Dis. 2026 Jan 9;17(1):20. [Abstract]
- Cell Death Dis. 2025 Jan 20;16(1):31. [Abstract]
- Cell Death Dis. 2023 Apr 20;14(4):280. [Abstract]
- Acta Pharmacol Sin. 2024 Jun;45(6):1201-1213. [Abstract]
- Antioxidants (Basel). 2022 Jun 27;11(7):1264. [Abstract]
- Cell Rep. 2025 Nov 25;44(11):116505. [Abstract]
- Kardiol Pol. 2021;79(9):972-979. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jun 1:257:114940. [Abstract]
- Ecotoxicol Environ Saf. 2022 May 1;236:113454. [Abstract]
- Biochem Pharmacol. 2023 Nov:217:115816. [Abstract]
- Cancer Biol Ther. 2018;19(12):1193-1203. [Abstract]
- Toxicology. 2024 Nov 9:509:153994. [Abstract]
- Chem Biol Interact. 2021 Oct 1:348:109625. [Abstract]
- J Mol Med (Berl). 2023 Dec;101(12):1567-1585. [Abstract]
- Oncol Rep. 2021 Jan;45(1):83-94. [Abstract]
- FASEB J. 2020 Jan;34(1):1481-1496. [Abstract]
- J Virol. 2025 Feb 25;99(2):e0140824. [Abstract]
- Endocrinology. 2021 Aug 1;162(8):bqab077. [Abstract]
- J Breast Cancer. 2019 Jun;22(2):185-195. [Abstract]
- Exp Cell Res. 2024 Mar 1;436(1):113956. [Abstract]
- Cell Mol Bioeng. 2022 Oct 6;15(6):599-609. [Abstract]
- Life Sci Alliance. 2024 Oct 28;8(1):e202402585. [Abstract]
- Biochem Biophys Res Commun. 2019 Oct 29;519(1):134-140. [Abstract]
- Microcirculation. 2021 May;28(4):e12680. [Abstract]
- Anticancer Drugs. 2025 Oct 16. [Abstract]
- bioRxiv. 2025 Mar 4:2025.02.27.640687. [Abstract]
- SSRN. 2024 Feb 13.
- bioRxiv. 2023 Oct 16.
Customer Validation & Images
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Biological Activity
Kd: 0.4 uM (RhoA)[1]
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 (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.
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Animal Model:D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background[3]
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Dosage:40 mg/kg
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Administration:i.p.
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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.
Chemical Information
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CAS No. 1173671-63-0
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Appearance Solid
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Molecular Weight 358.40
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Formula C20H18N6O
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Color Light yellow to brown
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SMILES
O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (39)
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Journal Impact Factor
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Most Recent
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Nature
2025 Sep;645(8079):244-253. PMID: 40562926
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.
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Circulation
Dietary Geranylgeranyl Pyrophosphate Counteracts the Benefits of Statin Therapy in Experimental Pulmonary Hypertension. [Abstract]2021 May 4;143(18):1775-1792. PMID: 33660517
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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Cancer Res
An In Vivo CRISPR Screen Identifies Stepwise Genetic Dependencies of Metastatic Progression. [Abstract]2022 Feb 15;82(4):681-694. PMID: 34916221 -
Nat Commun
Smoking aggravates neovascular age-related macular degeneration via Sema4D-PlexinB1 axis-mediated activation of pericytes. [Abstract]2025 Mar 22;16(1):2821. PMID: 40121188
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.
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Nat Commun
Deficiency of gluconeogenic enzyme PCK1 promotes metabolic-associated fatty liver disease through PI3K/AKT/PDGF axis activation in male mice. [Abstract]2023 Mar 14;14(1):1402. PMID: 36918564
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.
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Exp Mol Med
Acetylation of α-tubulin restores endothelial cell injury and blood-brain barrier disruption after intracerebral hemorrhage in mice. [Abstract]2025 May;57(5):1064-1077. PMID: 40335634 -
Neuron
2025 Nov 26:S0896-6273(25)00842-6. PMID: 41308645 -
Redox Biol
Human lung microvascular endothelial cell protein modification by 2-chlorohexadecanoic acid: RhoA mediates 2-chlorohexadecanoic acid-elicited endothelial activation. [Abstract]2025 May:82:103596. PMID: 40117888 -
Theranostics
PTBP1 knockdown promotes neural differentiation of glioblastoma cells through UNC5B receptor. [Abstract]2022 May 9;12(8):3847-3861. PMID: 35664063 -
J Clin Invest
2025 Jun 2;135(11):e184158. PMID: 40454481 -
Cell Death Dis
Loss of PRKACB facilitates metastasis of diffuse-type gastric cancer through RhoA signaling activation. [Abstract]2026 Mar 18;17(1):281. PMID: 41851075 -
Cell Death Dis
VIRMA/IGF2BP3-mediated ANLN upregulation promotes intrahepatic cholangiocarcinoma growth by forming a positive feedback loop with RhoA/YAP1/TEAD1 signaling pathway. [Abstract]2026 Jan 9;17(1):20. PMID: 41513610 -
Cell Death Dis
S1PR3-driven positive feedback loop sustains STAT3 activation and keratinocyte hyperproliferation in psoriasis. [Abstract]2025 Jan 20;16(1):31. PMID: 39833165 -
Cell Death Dis
Septin11 promotes hepatocellular carcinoma cell motility by activating RhoA to regulate cytoskeleton and cell adhesion. [Abstract]2023 Apr 20;14(4):280. PMID: 37080972 -
Acta Pharmacol Sin
Angiotensin II type-2 receptor signaling facilitates liver injury repair and regeneration via inactivation of Hippo pathway. [Abstract]2024 Jun;45(6):1201-1213. PMID: 38491160 -
Antioxidants (Basel)
Selenoprotein K Is Essential for the Migration and Phagocytosis of Immature Dendritic Cells. [Abstract]2022 Jun 27;11(7):1264. PMID: 35883755 -
Cell Rep
Tunneling nanotube-mediated stem cell immunomodulation dysfunction promotes adipose inflammation and insulin resistance in GDM. [Abstract]2025 Nov 25;44(11):116505. PMID: 41187060 -
Kardiol Pol
Src-IL-18 signaling regulates the secretion of atrial natriuretic factor in hypoxic beating rat atria. [Abstract]2021;79(9):972-979. PMID: 34176112 -
Ecotoxicol Environ Saf
Fluoride disrupts intestinal epithelial tight junction integrity through intracellular calcium-mediated RhoA/ROCK signaling and myosin light chain kinase. [Abstract]2023 Jun 1:257:114940. PMID: 37099960 -
Ecotoxicol Environ Saf
Long-term exposure to low concentrations of MC-LR induces blood-testis barrier damage through the RhoA/ROCK pathway. [Abstract]2022 May 1;236:113454. PMID: 35367887 -
Biochem Pharmacol
TIPE2 ameliorates neuroinflammation and cognitive impairment in sepsis-associated encephalopathy through regulating RhoA/ROCK2-NF-κB signaling pathway. [Abstract]2023 Nov:217:115816. PMID: 37748665 -
Cancer Biol Ther
2018;19(12):1193-1203. PMID: 30081723 -
Toxicology
Bisphenol A disrupts the neuronal F-actin cytoskeleton by activating the RhoA/ROCK/LIMK pathway in Neuro-2a cells. [Abstract]2024 Nov 9:509:153994. PMID: 39527977 -
Chem Biol Interact
Catalpol ameliorates endothelial dysfunction and inflammation in diabetic nephropathy via suppression of RAGE/RhoA/ROCK signaling pathway. [Abstract]2021 Oct 1:348:109625. PMID: 34416245 -
J Mol Med (Berl)
Vav2 promotes ductus arteriosus anatomic closure via the remodeling of smooth muscle cells by Rac1 activation. [Abstract]2023 Dec;101(12):1567-1585. PMID: 37804474 -
Oncol Rep
Platelet‑derived growth factor‑BB mediates pancreatic cancer malignancy via regulation of the Hippo/Yes‑associated protein signaling pathway. [Abstract]2021 Jan;45(1):83-94. PMID: 33416116 -
FASEB J
Par6 regulates cell cycle progression through enhancement of Akt/PI3K/GSK-3β signaling pathway activation in glioma. [Abstract]2020 Jan;34(1):1481-1496. PMID: 31914615 -
J Virol
Tetraspanin CD81 serves as a functional entry factor for porcine circovirus type 2 infection. [Abstract]2025 Feb 25;99(2):e0140824. PMID: 39745447 -
Endocrinology
2021 Aug 1;162(8):bqab077. PMID: 33851697 -
J Breast Cancer
Doxorubicin Promotes Migration and Invasion of Breast Cancer Cells through the Upregulation of the RhoA/MLC Pathway. [Abstract]2019 Jun;22(2):185-195. PMID: 31281722 -
Exp Cell Res
Inhibition of RhoGEF/RhoA alleviates regorafenib resistance and cancer stemness via Hippo signaling pathway in hepatocellular carcinoma. [Abstract]2024 Mar 1;436(1):113956. PMID: 38341081 -
Cell Mol Bioeng
Light Activates Cdc42-Mediated Needle-Shaped Filopodia Formation via the Integration of Small GTPases. [Abstract]2022 Oct 6;15(6):599-609. PMID: 36531863 -
Life Sci Alliance
Decoupling actin assembly from microtubule disassembly by TBC1D3C-mediated direct GEF-H1 activation. [Abstract]2024 Oct 28;8(1):e202402585. PMID: 39467635 -
Biochem Biophys Res Commun
Cdc42-mediated supracellular cytoskeleton induced cancer cell migration under low shear stress. [Abstract]2019 Oct 29;519(1):134-140. PMID: 31477271 -
Microcirculation
Post-treatment with yiqifumai injection and its main ingredients attenuates lipopolysaccharide-induced microvascular disturbance in mesentery and ileum. [Abstract]2021 May;28(4):e12680. PMID: 33486837 -
Anticancer Drugs
A genome-wide screen identified ARHGAP35 as a regulator of regorafenib resistance in liver cancer. [Abstract]2025 Oct 16. PMID: 41176659 -
bioRxiv
RHOA Loss of Function Impairs the IFNγ Response and Promotes CD19 Antigen Escape to Drive CAR-T Resistance in Diffuse Large B-cell Lymphoma. [Abstract]2025 Mar 4:2025.02.27.640687. PMID: 40093149 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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 |
Rhosin Related Classifications
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