Catalog No.: PC-25791Not For Human Use, Lab Use Only.
(6R)-HR3119 is a small molecule ligand of Guanine nucleotide dissociation inhibitors (GDIs) protein RhoGDI2 with low-micromolar affinity (Kd= 4 uM), engages with RhoGDI2 in cells and suppresses the migration of aggressive breast cancer cells.
(6R)-HR3119 is a small molecule ligand of Guanine nucleotide dissociation inhibitors (GDIs) protein RhoGDI2 with low-micromolar affinity (Kd= 4 uM), engages with RhoGDI2 in cells and suppresses the migration of aggressive breast cancer cells.
(6R)-HR3119 shows a modest level of selectivity over RhoGDI1 (>7-fold, Kd = 31 μM), and displays greater selectivity against PDEδ (>30-fold.
(6R)-HR3119 stabilized RhoGDI2 in MDA-MB-231 cells, more effectively than (6S)-HR3119.
RhoGDI2 plays a dual role in the regulation of Rho GTPases, both forming stable complexes with Rho GTPases to maintain their inactive state and serving as a chaperone to protect them from proteasomal degradation and facilitate the transport of inactive Rho GTPases to membranes for subsequent activation.
