Rhosin hydrochloride

Research use only, not for human use.

Rhosin hydrochloride is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM).

Rhosin hydrochloride is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin hydrochloride does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride causes cell apoptosis.

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.

Rhosin (40 mg/kg; i.p.) treatment prevents social avoidance caused by social defeat stress. Rhosin also blocks sucrose preference deficits induced by defeat in C57Bl6/J (Jackson) mice.?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. Animal Model:D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background Dosage:40 mg/kg Administration:I.p.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.

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Apoptosis

Apoptosis

Apoptosis|RhoA

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1281870-42-5

394.86

C20H19ClN6O

>98% (HPLC)

DMSO:100 mg/mL (253.25 mM; Need ultrasonic)

O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4.Cl

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(-20℃)

With Ice Pack

≥ 2 years