YM-254890 | Gαq inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 100 ug | $65.00 | ||
| 1 mg | $340.00 |
YM-254890 (568580-02-9) 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
References/Citations:
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 42
5) Kankanamge et al. (2018) Melanopsin (Opn4) utilizes Gαi Gβγ as major signal transducers; J. Cell Sci., 131 Jcs212910 [Focus Citation]
6) Pera et al. (2018) Biased signaling of the proton-sensing receptor OGR1 by benzodiazepines; FASEB J., 32 862[Focus Citation]
7) Ratnayake et al. (2018) Blue light excited retina intercepts cellular signaling; Sci. Rep. 8 10207[Focus Citation]
8) 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]
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
YM-254890 (568580-02-9) 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
References/Citations:
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 42
5) Kankanamge et al. (2018) Melanopsin (Opn4) utilizes Gαi Gβγ as major signal transducers; J. Cell Sci., 131 Jcs212910 [Focus Citation]
6) Pera et al. (2018) Biased signaling of the proton-sensing receptor OGR1 by benzodiazepines; FASEB J., 32 862[Focus Citation]
7) Ratnayake et al. (2018) Blue light excited retina intercepts cellular signaling; Sci. Rep. 8 10207[Focus Citation]
8) 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]
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