Products Details

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

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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