Y16 is an inhibitor of G-protein–coupled Rho GEFs and works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.
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Y16 acts as a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd of 76 nM. It effectively inhibits the interaction between LARG and associated G-protein-coupled Rho GEFs with RhoA. Y16 does not impact other members of the diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP[1].
体外研究
Y16 (10-30 µM; 24 hours; NIH 3T3 cells) inhibits the formation of RhoA-GTP induced by serum in a dose-dependent manner and specifically targets RhoA[1].
Y16 (10-30 µM; 24 hours; NIH 3T3 cells) effectively blocks the formation of phospho-MLC and phospho-FAK induced by serum or SDF-1α, both of which are downstream of RhoA[1].
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