Rhosin (hydrochloride)

Rhosin is an inhibitor of the protein-protein interaction between Rho and guanine nucleotide exchange factors (GEFs).¹ It inhibits RhoA activity when used at concentrations of 10 and 30 µM and selectively reduces the number and size of MCF-7 breast cancer cell mammospheres over MCF-10A non-cancerous cell mammospheres. It also inhibits migration and invasion of MCF-7 cells and human mammary epithelial cells expressing RhoC. Rhosin (30 µM) increases neurite outgrowth in PC12 cells. It prevents social defeat stress-induced hyperexcitability and increases spine density in nucleus accumbens dopamine 1 receptor medium spiny neurons (D1-MSNs) when administered post-social defeat stress in a mouse model of depression at a dose of 40 mg/kg.² It also prevents social defeat stress-induced social avoidance and reductions in sucrose preference in the same model.

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1. Shang, X., Marchioni, F., Sipes, N., et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem. Biol. 19(6), 699-710 (2012).

2. Francis, T.C., Gaynor, A., Chandra, R., et al. The selective RhoA inhibitor rhosin promotes stress resiliency through enhancing D₁-medium spiny neuron plasticity and reducing hyperexcitability. Biol. Psychiatry 85(12), 1001-1010 (2019).