Name | Rhosin (hydrochloride) |
Synonyms | Rhosin HCl G04 HYDROCHLORIDE Rhosin (hydrochloride) D-Tryptophan (2E)-2-(6-quinoxalinylmethylene)hydrazide hydrochloride (R,E)-2-amino-3-(1H-indol-3-yl)-N'-(quinoxalin-6-ylmethylene)propanehydrazide hydrochloride (2R)-2-amino-3-(1H-indol-3-yl)-N'-[(quinoxalin-6-yl)methylidene]propanehydrazide hydrochloride |
CAS | 1281870-42-5 |
Molecular Formula | C20H19ClN6O |
Molar Mass | 394.86 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
In vitro study | Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC 50 ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.533 ml | 12.663 ml | 25.326 ml |
5 mM | 0.507 ml | 2.533 ml | 5.065 ml |
10 mM | 0.253 ml | 1.266 ml | 2.533 ml |
5 mM | 0.051 ml | 0.253 ml | 0.507 ml |
biological activity | Rhosin (G04) hydrochloride (HCl) is a potent and specific inhibitor of the RhoA subfamily Rho GTPases, the Kd value was approximately 0.4 uM. Rhosin hydrochloride can induce apoptosis. |
Target | Value |
Rho (Cell-free assay) | 0.4 μM(Kd) |
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. |