| Name | TUG-891 |
| Description | TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. |
| Kinase Assay | Inhibition of recombinant human Mps1 by BAY 1161909 or BAY 1217389 is assessed in TRFRET-based in vitro kinase assays via phosphorylation of a biotinylated peptide (Biotin-Ahx-PWDPDDADITEILG-NH2). Under standard assay conditions kinase and test compound are preincubated for 15 min before enzyme reaction is started by addition of substrate and ATP upon 10 μM[1]. |
| In vitro | TUG-891 exhibits analogous signaling characteristics to the long-chain fatty acid (LCFA) α-linolenic acid at the human Free Fatty Acid receptor 4 (FFA4), stimulating Ca2+ mobilization, recruiting β-arrestin-1 and β-arrestin-2, and promoting extracellular signal-regulated kinase phosphorylation. Moreover, TUG-891 activation of FFA4 leads to the receptor's swift phosphorylation and internalization[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.49 mM), Sonication is recommended. DMSO : 250 mg/mL (686.04 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | TUG-891 | Inhibitor | inhibit | GPR120 | Free Fatty Acid Receptor | FFAR |
| Inhibitors Related | Monomethyl fumarate | Pamoic acid disodium | Azathioprine | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | TUG-424 | Timapiprant | Tricosanoic acid |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | GPCR Compound Library | Anti-Metabolism Disease Compound Library | Anti-Cancer Compound Library | Human Metabolite Library |