Chemical Structure : (6R)-HR3119
CAS No.:
(6R)-HR3119
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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
(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.
Physicochemical Properties
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M.Wt
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437.53
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Formula
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C24H24FN3O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(2-(((R)-(2'-fluoro-[1,1'-biphenyl]-4-yl)(thiophen-2-yl)methyl)amino)-2-oxoethyl)pyrrolidine-3-carboxamide
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References
1. Mingqing Liu, et al. ACS Chem Biol. 2025 Nov 21;20(11):2584-2592.
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