YM-254890
Gq inhibitor / YM-254890 is a novel Gαq/11 inhibitor,1 U46619-induced platelet aggregation is inhibited but phorbol ester- or ionophore-induced aggregation is not2 (IC50 = 0.1-0.2 μM)1. It blocks Pasteurella multocida toxin-mediated activation of Gαq.3 A highly useful new tool for studying Gαq/11-coupled receptor signaling and resulting cellular events.4
Biochemicals & reagents
568580-02-9
1) Takasaki (2004), A novel Galphaq/11-selective inhibitor; J. Biol. Chem., 279 47438 2) Uemura et al. (2006), Biological properties of a specific Galpha q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress; Br. J. Pharmacol., 148 61 3) Orth et al. (2005), Pasteurella multocida toxin-induced activation of RhoA is mediated via two families of G{alpha} proteins, G{alpha}g and G{alpha}12/13; J. Biol. Chem., 280 36701 4) Mizuno and Itoh (2009), Functions and regulatory mechanisms of Gq-signaling pathways; Neurosignals, 17 42b 5) Zimering and Nadkami (2019) Schizophrenia Autoantibodies Promote “Biased agonism” at the 5-Hydroxytryptamine 2A Receptor: Neurotoxicity is Positively Modulated by Metabotropic Glutamate 2/3 Receptor Agonism; Endocrinol. Diabetes Metab. J., 3 1 [Focus Citation]
-20°C
TARGET: GPCR -- PATHWAY: Coagulation; Proliferation; Cytokine -- DISEASE AREA: Cancer