| CAS NO: | 2103-64-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 364.31 |
| Cas No. | 2103-64-2 |
| Formula | C20H12O7 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥18.1 mg/mL in DMSO |
| Chemical Name | 3',4',5',6'-tetrahydroxy-3H-spiro[isobenzofuran-1,9'-xanthen]-3-one |
| Canonical SMILES | O=C1O[C@]2(C(C=CC(O)=C3O)=C3OC4=C2C=CC(O)=C4O)C5=CC=CC=C51 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Gallein is a small inhibitor of G protein βγ (Gβγ) subunit signalling [1].
Gβγ subunits are central participants in G protein-coupled receptor (GPCR) signaling pathways. Gβγ subunits interact with receptors, G protein α subunits and downstream targets to coordinate multiple, different GPCR functions [2].
In spheroids made by LNCaP cells and grown in collagen gels, gallein at 10 μM was able to significantly counteract β-ionone-induced LNCaP cell invasiveness [1]. In human monocyte-derived macrophages, gallein effectively inhibited M1 polarization and promoted M2 polarization [3].
In castrated male NSG mice carrying subcutaneous injected LNCaP cells, intraperitoneal injection of gallein (5 mg/kg/day) inhibited β-ionone-mediated metastasis spread [1]. In a rat model of autoimmune myocarditis, gallein (10 mg/kg/day, p.o., for 21 days) effectively improved survival and cardiac function, suppressed cardiac remodeling, and further attenuated myocardial protein expression of G protein-coupled receptor kinase 2 (GRK2) as well as high mobility group box 1 (HMGB1) and its cascade signaling proteins [3].
References:
[1]. Sanz G, Leray I, Muscat A, et al. Gallein, a Gβγ subunit signalling inhibitor, inhibits metastatic spread of tumour cells expressing OR51E2 and exposed to its odorant ligand. BMC Research Notes, 2017, 10(1): 541.
[2]. Smrcka A V. G protein βγ subunits: central mediators of G protein-coupled receptor signaling. Cellular and Molecular Life Sciences, 2008, 65(14): 2191-2214.
[3]. Karuppagounder V, Bajpai A, Meng S, et al. Small molecule disruption of G protein βγ subunit signaling reprograms human macrophage phenotype and prevents autoimmune myocarditis in rats. PLoS One, 2018, 13(7): e0200697.
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