555460-M

Rhosin

≥93% (HPLC), powder, Rho inhibitor, Calbiochem^®

• Synonym(s): Rho Inhibitor, Rhosin, G04, (2 R)-2-Amino-3-(1H-indol-3-yl)-Nʹ-((1 E)-quinoxalin-6-ylmethylidene)propanehydrazide, G04, (2R)-2-Amino-3-(1H-indol-3-yl)-Nʹ-((1E)-quinoxalin-6-ylmethylidene)propanehydrazide
• Empirical Formula (Hill Notation): C₂₀H₁₈N₆O
• CAS Number: 1173671-63-0
• Molecular Weight: 358.40
• UNSPSC Code: 12352200

Properties

• product name: Rho Inhibitor, Rhosin, Rho Inhibitor, Rhosin, CAS 1173671-63-0, is a cell-permeable compound that directly targets Rho GEF binding domain (Kd = 354 nM for RhoA), thereby prevents Rho from interacting with its GEFs.
• Quality Level: 100
• Assay: ≥93% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange-brown
• solubility: DMSO: 10 mg/mL
• storage temp.: 2-8°C

Description

General description

Rhosin is composed of two aromatic rings connected by a linker and binds to the area surrounding Trp58 of RhoA with a Kd in the submicromolar range, effectively inhibiting GEF-catalyzed RhoA activation. This compound is valuable for studying the physiological role of RhoA subfamily GTPases and assessing the therapeutic potential of targeting Rho in pathological conditions.
Moreover, Rhosin can inhibit YAP activation by targeting RhoA and RhoC. It can also suppress tumor cell metastasis by inhibiting the Rho/YAP pathway and modulating the expression of RHAMM and CXCR4 in melanoma and breast cancer cells. It promotes stress resilience by enhancing D1-MSN plasticity and reducing hyperexcitability.

Application

Rho Inhibitor, Rhosin has been used to treat single breast tumor cells to regulate RhoA activity to validate the cell line with the Förster resonance energy transfer (FRET) biosensor.

Biochem/physiol Actions

Primary Target
Rho GTPase

Target K_i: 354 nM for RhoA

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Shang, X., et al. 2012. Chem. Biol.19, 699.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable