Rhosin hydrochloride

Catalog No.S8988 Batch:S898801

Technical Data

Formula	C₂₀H₁₉ClN₆O
Molecular Weight	394.86	CAS No.	1281870-42-5
Solubility (25°C)*	In vitro	DMSO	93 mg/mL (235.52 mM)
		Water	93 mg/mL (235.52 mM)
		Ethanol	46 mg/mL (116.49 mM)
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[2]}	Animal Models 8-week-old female Balb/c mice, 8-week-old female C57BL/6J mice Dosages 10 mg/kg, 30 mg/kg Administration --

Cell Assay:^{^[1]}

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.

Animal Study:^{^[2]}

Animal Models
8-week-old female Balb/c mice, 8-week-old female C57BL/6J mice
Dosages
10 mg/kg, 30 mg/kg
Administration
--

References

Selleck's Rhosin hydrochloride has been cited by 2 publications

Inhibition of exchange proteins directly activated by cAMP as a strategy for broad-spectrum antiviral development [ J Biol Chem, 2023, 299(6):104749]	PubMed: 37100284
YAP1 activation promotes epithelial-mesenchymal transition and cell survival of renal cell carcinoma cells under shear stress [ Carcinogenesis, 2022, bgac014]	PubMed: 35147702

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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