Rhosin hydrochloride (Synonyms: G04) |
| Catalog No.GC32729 |
Le chlorhydrate de rhodine est un inhibiteur puissant et spécifique des Rho GTPases de la sous-famille RhoA. Le chlorhydrate de rhodine se lie spécifiquement À RhoA pour inhiber l'interaction RhoA-GEF avec un Kd d'environ 0,4 uM, et n'interagit pas avec Cdc42 ou Rac1, ni le GEF, LARG. Le chlorhydrate de rhodine induit l'apoptose cellulaire. Le chlorhydrate de rhodine favorise la résilience au stress en améliorant la plasticité D1-MSN et en réduisant l'hyperexcitabilité.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1281870-42-5
Sample solution is provided at 25 µL, 10mM.
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Rhosin Hcl is a specific Rho inhibitor; binds to WT RhoA with an affinity ~0.4 uM Kd; does not interfere with the binding of Cdc42 or Rac1.IC50 value: 0.4 uM(binding Kd) [1]Target: RhoA inhibitorRhosin is specific to the interaction between RhoA and its GEFs including LARG, DBL, LBC, p115 RhoGEF or PDZ RhoGEF and does not interfere with the binding of Cdc42 or Rac1 to their respective GEFs. Rhosin showed a dose-dependent inhibition of endogenous RhoA activity and cell growth of MCF7 cells. Rhosin dose-dependently reduced RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50μM, and caused decreased size and reduced number of mammospheres in MCF7 cells [1]. Y16 works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions [2].
[1]. Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710. [2]. Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60.
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