555460-M

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.

• 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

• 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

A cell-permeable (quinoxalinylmethylidene-D-Tryptophanyl)hydrazide that directly targets Rho GEF binding domain (Kd = 354 nM for RhoA), thereby prevents Rho from interacting with its GEFs (including LARG, DBL, LBC, p115 RhoGEF, and PDZ RhoGEF), but not p190RhoGAP, RhoGDI, or its effectors (ROCK, mDia, PKN, Rhoteckin). Shown to inhibit serum-induced RhoA, RhoB, and RhoC, but not Cdc42 or Rac1, activation, MLC & PAK phosphorylation, as well as stress fiber & focal complex formation in serum-starved NIH3T3 cultures (Effective conc. 30 µM) in a reversible manner.

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