Gallein

Gallein

Catalog Number:
L002372308APE
Mfr. No.:
APE-B7271
Price:
$175
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          3',4',5',6'-tetrahydroxy-3H-spiro[isobenzofuran-1,9'-xanthen]-3-one
          CAS Number
          2103-64-2
          Molecular Formula
          C20H12O7
          Molecular Weight
          364.31
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in EtOH; insoluble in H2O; ≥18.1 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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