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首页-小分子抑制剂&激动剂-Others-Small GTPase-(6R)-HR3119
(6R)-HR3119

Chemical Structure : (6R)-HR3119

CAS No.:

(6R)-HR3119

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

(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.

物理化学性质&存储条件

分子量 437.53
分子式 C24H24FN3O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(((R)-(2'-fluoro-[1,1'-biphenyl]-4-yl)(thiophen-2-yl)methyl)amino)-2-oxoethyl)pyrrolidine-3-carboxamide

参考文献

1. Mingqing Liu, et al. ACS Chem Biol. 2025 Nov 21;20(11):2584-2592.

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