Rhosin hydrochloride
Based on 39 publication(s) in Google Scholar
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride 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.
- Purity: 99.94%
- CAS No.: 1281870-42-5
- Formula: C20H19ClN6O
- Molecular Weight:394.86
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
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Publications Citing Use of MedChemExpress (MCE) Rhosin hydrochloride
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]
- Neuron. 2025 Nov 26:S0896-6273(25)00842-6. [Abstract]
- J Clin Invest. 2025 Jun 2;135(11):e184158. [Abstract]
- Theranostics. 2022 May 9;12(8):3847-3861. [Abstract]
- Exp Mol Med. 2025 May;57(5):1064-1077. [Abstract]
- Redox Biol. 2025 May:82:103596. [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]
- Cell Rep. 2025 Nov 25;44(11):116505. [Abstract]
- Antioxidants (Basel). 2022 Jun 27;11(7):1264. [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]
- Chem Biol Interact. 2021 Oct 1:348:109625. [Abstract]
- Cell Mol Bioeng. 2022 Oct 6;15(6):599-609. [Abstract]
- Toxicology. 2024 Nov 9:509:153994. [Abstract]
- Cancer Biol Ther. 2018;19(12):1193-1203. [Abstract]
- J Mol Med (Berl). 2023 Dec;101(12):1567-1585. [Abstract]
- FASEB J. 2020 Jan;34(1):1481-1496. [Abstract]
- Oncol Rep. 2021 Jan;45(1):83-94. [Abstract]
- J Virol. 2024 Dec 31:e0140824. [Abstract]
- Kardiol Pol. 2021;79(9):972-979. [Abstract]
- Exp Cell Res. 2024 Mar 1;436(1):113956. [Abstract]
- Endocrinology. 2021 Aug 1;162(8):bqab077. [Abstract]
- Life Sci Alliance. 2024 Oct 28;8(1):e202402585. [Abstract]
- J Breast Cancer. 2019 Apr 22;22(2):185-195. [Abstract]
- Anticancer Drugs. 2025 Oct 16. [Abstract]
- Biochem Biophys Res Commun. 2019 Oct 29;519(1):134-140. [Abstract]
- Microcirculation. 2021 May;28(4):e12680. [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 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].
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[3].
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. 1281870-42-5
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Appearance Solid
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Molecular Weight 394.86
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Formula C20H19ClN6O
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Color Light yellow to yellow
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SMILES
O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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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Neuron
2025 Nov 26:S0896-6273(25)00842-6. PMID: 41308645 -
J Clin Invest
2025 Jun 2;135(11):e184158. PMID: 40454481 -
Theranostics
PTBP1 knockdown promotes neural differentiation of glioblastoma cells through UNC5B receptor. [Abstract]2022 May 9;12(8):3847-3861. PMID: 35664063 -
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 -
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 -
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 -
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 -
Antioxidants (Basel)
Selenoprotein K Is Essential for the Migration and Phagocytosis of Immature Dendritic Cells. [Abstract]2022 Jun 27;11(7):1264. PMID: 35883755 -
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 -
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 -
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 -
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 -
Cancer Biol Ther
2018;19(12):1193-1203. PMID: 30081723 -
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 -
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 -
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 -
J Virol
Tetraspanin CD81 serves as a functional entry factor for porcine circovirus type 2 infection. [Abstract]2024 Dec 31:e0140824. PMID: 39745447 -
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 -
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 -
Endocrinology
2021 Aug 1;162(8):bqab077. PMID: 33851697 -
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 -
J Breast Cancer
Doxorubicin Promotes Migration and Invasion of Breast Cancer Cells through the Upregulation of the RhoA/MLC Pathway. [Abstract]2019 Apr 22;22(2):185-195. PMID: 31281722 -
Anticancer Drugs
A genome-wide screen identified ARHGAP35 as a regulator of regorafenib resistance in liver cancer. [Abstract]2025 Oct 16. PMID: 41176659 -
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 -
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 (126.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 16.67 mg/mL (42.22 mM; Need ultrasonic)
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (6.33 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 (6.33 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.5325 mL | 12.6627 mL | 25.3254 mL | 63.3136 mL |
| 5 mM | 0.5065 mL | 2.5325 mL | 5.0651 mL | 12.6627 mL | |
| 10 mM | 0.2533 mL | 1.2663 mL | 2.5325 mL | 6.3314 mL | |
| 15 mM | 0.1688 mL | 0.8442 mL | 1.6884 mL | 4.2209 mL | |
| 20 mM | 0.1266 mL | 0.6331 mL | 1.2663 mL | 3.1657 mL | |
| 25 mM | 0.1013 mL | 0.5065 mL | 1.0130 mL | 2.5325 mL | |
| 30 mM | 0.0844 mL | 0.4221 mL | 0.8442 mL | 2.1105 mL | |
| 40 mM | 0.0633 mL | 0.3166 mL | 0.6331 mL | 1.5828 mL | |
| DMSO | 50 mM | 0.0507 mL | 0.2533 mL | 0.5065 mL | 1.2663 mL |
| 60 mM | 0.0422 mL | 0.2110 mL | 0.4221 mL | 1.0552 mL | |
| 80 mM | 0.0317 mL | 0.1583 mL | 0.3166 mL | 0.7914 mL | |
| 100 mM | 0.0253 mL | 0.1266 mL | 0.2533 mL | 0.6331 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Rhosin hydrochloride Related Classifications
HY-12646 Related Classifications
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