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Gallein is an inhibitor of G protein βγ subunit-dependent signaling.1 It binds to Gβ1γ2 in a cell-free assay (IC50 = 200 nM) and inhibits Gβγ-dependent activation of PI3K in HL-60 cells. Gallein (10 µM) also inhibits Rac1 activation, superoxide production, and chemotaxis induced by N-formyl-Met-Leu-Phe (fMLP; Item No. 21495) in differentiated HL-60 cells. In vivo, gallein (10 mg/kg per day) increases survival, reduces ventricular hypertrophy, and attenuates cardiac remodeling in a mouse model of heart failure induced by transverse aortic constriction (TAC).2
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1. Small molecule disruption of G protein βγ subunit signaling inhibits neutrophil chemotaxis and inflammation. Mol. Pharmacol. 73(2), 410-418 (2008).
2. Simultaneous adrenal and cardiac G-