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Biological Data Biological description Gq- G-protein inhibitor which potently inhibits Gq/11 heterotrimeric G protein signaling by blocking GDP exchange of GTP on the α- subunit of the Gq complex. Recently reported to act as a broad-spectrum inhibitor for Gq- and Gs-proteins and exhibits a biased inhibition on Gi/o signaling, without affecting non-GPCR-mediated cellular signaling (Peng et al 2021). Shown to attenuate ADP-, collagen-, TRAP-, arachidonic acid- and U46619-induced platelet aggregation to show antithrombotic effects.
Solubility & Handling Storage instructions -20°C
Solubility overview Soluble in DMSO (10mg/ml)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use
Chemical Data Chemical name [(1R )-1-[(3S ,6S ,9S ,12S ,18R ,21S ,22R )-21-acetamido-18-benzyl-3-[(1R )-1-methoxyethyl]-4,9,10,12,16,22-hexamethyl-15-methylidene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentazacyclodocos-6-yl]-2-methylpropyl] (2S ,3R )-2-acetamido-3-hydroxy-4-methylpentanoate
Molecular Formula C46 H69 N7 O15
PubChem identifier 9919454
SMILES C[C@@H]1[C@@H](C(=O)O[C@@H](C(=O)N(C(=C)C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)O1)[C@@H](C)OC)C)[C@@H](C(C)C)OC(=O)[C@H]([C@@H](C(C)C)O)NC(=O)C)C)C)C)C)CC2=CC=CC=C2)NC(=O)C
Source Chromobacterium sp.
InChi InChI=1S/C46H69N7O15/c1-22(2)37(56)34(49-30(11)55)45(63)68-38(23(3)4)35-43(61)53(14)36(28(9)65-15)46(64)66-27(8)33(48-29(10)54)44(62)67-32(21-31-19-17-16-18-20-31)42(60)52(13)25(6)39(57)47-24(5)41(59)51(12)26(7)40(58)50-35/h16-20,22-24,26-28,32-38,56H,6,2
InChiKey QVYLWCAYZGFGNF-WBWCVGBTSA-N
References for YM-254890 References are publications that support the biological activity of the product
Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells Peng et al (2021) Eur J Pharmacol. 173706 : 891 Structural and Dynamical Basis of G Protein Inhibition by YM-254890 and FR900359: An Inhibitor in Action Tietze et al (2019) J Chem Inf Model. 59(10) : 4361-4373 Effect of YM-254890, a specific Galphaq/11 inhibitor, on experimental peripheral arterial disease in rats Uemura et al (2006) Eur J Pharmacol. 536(1-2) : 154-61 Biological properties of a specific Galpha q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress Uemura et al (2006) Br J Pharmacol. 148(1) : 61-9 Pharmacological properties of YM-254890, a specific G(alpha)q/11 inhibitor, on thrombosis and neointima formation in mice Kawasaki et al (2005) Thromb Haemost. 94(1) : 184-92.
Potent Gq/11 signaling inhibitor. Reported as Gq- G-protein inhibitor and broad-spectrum inhibitor for Gq - and Gs -proteins.
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