| Name | CYM-5541 |
| Description | CYM-5541 (ML249) is a selective and allosteric S1P3 receptor agonist. |
| Kinase Assay | Jump-In TI CHO-K cells stably expressing WT or mutant S1P3 are serum-starved for 4 hrs. They are then incubated at 4 °C for 30 min in the binding buffer containing 20 mM Tris-HCl (pH 7.5), 100 mM NaCl, 15 mM NaF, 0.5 mM EDTA, 1 mM Na3VO4, 0.5% fatty acid-free bovine serum albumin, and protease inhibitor mixture with 0.1 nM [33P]S1P and increasing concentrations of S1P, SPM-242, or CYM-5541. Cells are washed three times with cold binding buffer. Cell-bound radioactivity is measured by lysing the cells with 0.5% SDS followed by liquid scintillation counting. The raw data is normalized so that the level of [33P]S1P bound to each cell line (WT or mutant) in the absence of competing ligand is referenced as 100% for its own cell line[1]. |
| In vitro | CYM-5541 is a full agonist that achieves maximal ERK phosphorylation levels comparable to S1P, with an EC50 of 72-132 nM and high selectivity over other S1P receptor subtypes: S1P1 EC50 >10 μM, S1P2 EC50 >50 μM, S1P4 EC50 >50 μM, and S1P5 EC50 >25 μM. It exhibits no significant activity in the Ricerca profiling panel of 55 GPCRs, ion channels, and transporters. CYM-5541 enabled the identification of an allosteric site, with residue F263 being crucial for its affinity and efficacy, suggesting the presence of a unique hydrophobic pocket responsible for its S1P3 selectivity [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 27.8 mg/mL (87.85 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.32 mM), Sonication is recommended.
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| Keywords | S1PReceptor | S1P3 | S1P Receptor | ML-249 | ML 249 | Lysophospholipid Receptor | LPLReceptor | LPL Receptor | LPL | Inhibitor | inhibit | CYM-5541 | CYM5541 | CID17253208 | CID 17253208 |
| Inhibitors Related | LX-2931 | Tyloxapol | Sphingosine-1-phosphate | CYM50374 | ASP-4058 | CAY10444 | Ki16198 | Siponimod | CYM5181 | Poloxamer 407 | S1PR1 modulator 1 | MP-A08 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | Multi-Target Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
