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Rhosin hydrochloride is a rho GTPase inhibitor (Kd = 354 nM). Inhibits binding of RhoA to guanine nucleotide exchange factors (GEFs) including LARG, DBL, LBC, p115 RhoGEF and PDZ RhoGEF. Has no effect on the binding of Rac1 or Cdc42 to their respective GEFs. Suppresses RhoA/C-mediated breast cancer cell migration and invasion in vitro. Also induces neurite outgrowth in synergy with NGF.
| Cell Experiment | |
|---|---|
| Cell lines | B16BL6 cells and 4T1 cells (mouse melanoma and breast cancer cell lines) |
| Preparation method | B16BL6 cells and 4T1 cells were treated with rhosin at indicated concentration for 3 days. Cell viability was assessed by MTT assay. For wound healing assays, MDA-MB-231 and HCC1937 basal-like breast cancer cells were maintained in RPMI medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with Rhosin hydrochloride (30μM) for 24 hours. Rhosin hydrochloride significantly inhibited cell migration in wound healing assays, reducing migration in MDA-MB-231 and HCC1937 cells. Rhosin hydrochloride suppressed stress fiber formation in MDA-MB-231 cells. |
| Concentrations | 1-50 µM (for B16BL6 and 4T1 cells); 30 µM (for MDA-MB-231 and HCC1937 wound healing assay) |
| Incubation time | 3 days (for B16BL6 and 4T1 cells); 24 hours (for MDA-MB-231 and HCC1937 wound healing assay) |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6J mice (male, 10-12 weeks old) subjected to chronic social defeat stress model |
| Formulation | Rhosin was prepared in a 5% DMSO, 0.9% saline solution, gently warmed to dissolve. Vehicle contained a 5% DMSO solution in 0.9% saline. |
| Dosages | 40 mg/kg |
| Administration | Intraperitoneally (i.p.) administered 15 min prior to physical defeat. For post-defeat treatment, injections were administered one time per day for 7 days and social interaction was retested on day 8. |
| Molecular Weight | 394.86 |
| Formula | C20H18N6O.HCl |
| CAS Number | 1281870-42-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL Water 17 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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