Rhosin hydrochloride

For research use only.

Catalog No.S8988 Synonyms: G04 hydrochloride, Rhosin HCl

Rhosin hydrochloride Chemical Structure

CAS No. 1281870-42-5

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.

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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 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]

In vivo

Treatment with rhosin abrogates the lung metastasis of B16BL6 and 4T1 cells in vivo.[2]

Protocol

Cell Research:

[1]

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  • 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 inhibitors (2 mM PMSF, 10 μg/ml leupeptin, 10 μg/ml aprotinin). 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.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: 8-week-old female Balb/c mice, 8-week-old female C57BL/6J mice
  • Dosages: 10 mg/kg, 30 mg/kg
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (235.52 mM)
Water 93 mg/mL (235.52 mM)
Ethanol ''''46 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 394.86
Formula

C20H19ClN6O

CAS No. 1281870-42-5
Storage powder
in solvent
Synonyms G04 hydrochloride, Rhosin HCl
Smiles C1=CC=C2C(=C1)C(=CN2)CC(C(=O)NN=CC3=CC4=NC=CN=C4C=C3)N.Cl

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID