Home Cell Cycle Rho inhibitor - Apoptosis related activator Rhosin hydrochloride For research use only.

Rhosin hydrochloride

Synonyms: G04 hydrochloride, Rhosin HCl

Rhosin (G04) hydrochloride (HCl) is a potent, specific inhibitor of RhoA subfamily Rho GTPases with Kd of ~ 0.4 uM. Rhosin hydrochloride induces cell apoptosis.

Rhosin hydrochloride Chemical Structure

Rhosin hydrochloride Chemical Structure

CAS No. 1281870-42-5

Purity & Quality Control

Rhosin hydrochloride Related Products

Signaling Pathway

Rho Signaling Pathways

Rho Signaling Pathway

Biological Activity

Description Rhosin (G04) hydrochloride (HCl) is a potent, specific inhibitor of RhoA subfamily Rho GTPases with Kd of ~ 0.4 uM. Rhosin hydrochloride induces cell apoptosis.
Targets
Rho [1]
(Cell-free assay)
0.4 μM(Kd)
In vitro
In vitro

In cells Rhosin specifically inhibits RhoA activity and RhoA-mediated cellular function without affecting Cdc42 or Rac1 signaling activities. By suppressing RhoA or RhoC activity Rhosin can inhibit mammary sphere formation by breast cancer cells, suppress invasion of mammary epithelial cells, and induce neurite outgrowth of PC12 cells in synergy with NGF.[1]
Cell Research Cell lines NIH3T3 cells, MCF7 cells, HME cells
Concentrations 10 μM, 30 μM, 50 μM
Incubation Time 24 h
Method

NIH3T3 cells, MCF7 cells, or HME cells are grown in log phase in a 10-cm dish or a sixwell dish, and are starved in serum-free medium in the presence or absence of G04 at indicated concentrations for 24 hours and are subsequently stimulated with 10% calf serum or fetal bovine serum for 15 min. Cells are lysed in a buffer containing 20 mM Tris-HCL, pH 7.6, 100 mM NaCl, 1% Triton X-100, 10 mM MgCl2, 2 mM NaF and protease inhibitor. Lysates are clarified, the protein concentrations are normalized, and the GTP-bound RhoA, Rac1 or Cdc42 in the lysates are measured by respective anti-RhoA, Rac1 and Cdc42 Western blotting of the effector domain pull-downs.
In Vivo
In vivo

Treatment with rhosin abrogates the lung metastasis of B16BL6 and 4T1 cells in vivo.[2]
Animal Research Animal Models 8-week-old female Balb/c mice, 8-week-old female C57BL/6J mice
Dosages 10 mg/kg, 30 mg/kg
Administration --

Chemical Information & Solubility

Molecular Weight 394.86 Formula

C20H19ClN6O
CAS No. 1281870-42-5 SDF --
Smiles C1=CC=C2C(=C1)C(=CN2)CC(C(=O)NN=CC3=CC4=NC=CN=C4C=C3)N.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 89 mg/mL ( (225.39 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 39 mg/mL

Ethanol : Insoluble


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In vivo
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