L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone

Description

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

Uses

YM-254890 is a selective inhibitor of Gαq.

storage

Store at -20°C

References

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]