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[1][2]. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3].
Product Specifications
CAS Number
1173671-63-0
UNSPSC
12352005
Hazard Statement
H315, H319, H320
Target
Apoptosis; Ras
Type
Reference compound
Related Pathways
Apoptosis; GPCR/G Protein; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Rhosin.html
Concentration
10mM
Purity
98.74
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4
Molecular Formula
C20H18N6O
Molecular Weight
358.40
Precautions
H315, H319, H320
References & Citations
[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.|[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Citation 01
Anticancer Drugs. 2025 Oct 16.|Antioxidants (Basel) . 2022 Jun 27;11 (7) :1264.|Biochem Biophys Res Commun. 2019 Oct 29;519 (1) :134-140.|Cancer Res. 2022 Feb 15;82 (4) :681-694.|Cell Death Dis. 2023 Apr 20;14 (4) :280.|Cell Mol Bioeng. 2022 Oct 6;15 (6) :599-609.|Cell Rep. 2025 Nov 25;44 (11) :116505.|Chem Biol Interact. 2021 Oct 1:348:109625.|Eur J Med Res. 2025 Nov 26;30 (1) :1187.|Exp Cell Res. 2024 Mar 1;436 (1) :113956.|J Breast Cancer. 2019 Apr 22;22 (2) :185-195. |Neuron. 2025 Nov 26:S0896-6273 (25) 00842-6.|SSRN. 2024 Feb 13.|Acta Pharmacol Sin. 2024 Jun;45 (6) :1201-1213.|Biochem Pharmacol. 2023 Nov:217:115816.|bioRxiv. 2023 Oct 16.|bioRxiv. 2025 Mar 4:2025.02.27.640687.|Cancer Biol Ther. 2018;19 (12) :1193-1203.|Cell Death Dis. 2025 Jan 20;16 (1) :31.|Circulation. 2021 May 4;143 (18) :1775-1792.|Ecotoxicol Environ Saf. 2022 May 1;236:113454.|Ecotoxicol Environ Saf. 2023 Jun 1:257:114940.|Endocrinology. 2021 Aug 1;162 (8) :bqab077.|Exp Mol Med. 2025 May;57 (5) :1064-1077.|FASEB J. 2020 Jan;34 (1) :1481-1496.|J Clin Invest. 2025 Jun 2;135 (11) :e184158.|J Mol Med (Berl) . 2023 Dec;101 (12) :1567-1585.|J Virol. 2024 Dec 31:e0140824.|Kardiol Pol. 2021;79 (9) :972-979.|Life Sci Alliance. 2024 Oct 28;8 (1) :e202402585.|Microcirculation. 2021 May;28 (4) :e12680.|Nat Commun. 2023 Mar 14;14 (1) :1402.|Nat Commun. 2025 Mar 22;16 (1) :2821.|Nature. 2025 Sep;645 (8079) :244-253.|Oncol Rep. 2021 Jan;45 (1) :83-94.|Redox Biol. 2025 May:82:103596.|Theranostics. 2022 May 9;12 (8) :3847-3861.|Toxicology. 2024 Nov 9:509:153994.
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