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Product 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].
Web ID
– HY-12646A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C20H18N6O
Citations
– Antioxidants (Basel). 2022, 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. 06 October 2022.|Chem Biol Interact. 17 August 2021, 109625.|J Breast Cancer. 2019 Apr 22;22(2):185-195. |Biochem Pharmacol. 2023 Sep 23;115816.|bioRxiv. 2023 Oct 16.|Cancer Biol Ther. 2018;19(12):1193-1203. |Circulation. 2021 May 4;143(18):1775-1792.|Ecotoxicol Environ Saf. 2022 May 1;236:113454.|Ecotoxicol Environ Saf. 2023 Apr 24;257:114940.|Endocrinology. 2021 Apr 14;bqab077.|FASEB J. 2020 Jan;34(1):1481-1496.|J Mol Med (Berl). 2023 Oct 7.|Kardiol Pol. 2021 Jun 27.|Microcirculation. 2021 Jan 23;e12680.|Nat Commun. 2023 Mar 14;14(1):1402.|Oncol Rep. 2021 Jan;45(1):83-94.|Theranostics. 2022 May 9;12(8):3847-3861.
References
– [1]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.|[2]Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710.|[3]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.
CAS Number
– 1173671-63-0
Molecular Weight
– 358.40
SMILES
– O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;Ras
Pathway
– Apoptosis;GPCR/G Protein
Product type
– Reference compound
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