RHO INHIBITOR RHOSIN 1PC X 25MG

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.

A cell-permeable (quinoxalinylmethylidene-D-tryptophanyl)hydrazide that directly targets Rho GEF binding domain (K_d = 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 suppress mammospheres formation in MCF7, but not the non-tumorigenic MCF10A, cultures and inhibit serum-induced RhoA, RhoB, and RhoC, but not Cdc42 or Rac1, activation, MLC & PAK phosphorylation, as well as stress fiber and focal complex formation in serum-starved NIH3T3 cultures (Effective conc. 30 µM) in a reversible manner. RhoA inactivation by G04 treatment (30 µM) is also demonstrated to promote neurite outgrowth and branching from NGF-treated PC12 cells.

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