Definition
ChEBI: Rhosin is a D-tryptophan derivative obtained by formal condensation of the carboxy group of D-tryptophan with the amino group of (quinoxalin-6-yl)methylidenehydrazide. It directly targets the Rho GEF binding domain, thereby preventing Rho from interacting with its GEFs It has a role as a RhoA inhibitor, a RhoC inhibitor and an antineoplastic agent. It is a D-tryptophan derivative, a quinoxaline derivative and a hydrazone.
General Description
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.
