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CYM-5541

Catalog No. T3961 CAS 945128-26-7

Synonyms: CID-17253208, ML249, CYM 5541

CYM-5541 is a selective and allosteric S1P3 receptor agonist.

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CYM-5541, CAS 945128-26-7

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Purity: 98%

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Description	CYM-5541 is a selective and allosteric S1P3 receptor agonist.
Targets&IC50	S1P3:72-132 nM(EC50)
In vitro	CYM-5541 is a full agonist, able to reach the maximum level of ERK phosphorylation that is observed with S1P. CYM-5541 has an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes: S1P1 EC50>10 μM, S1P2 EC50>50 μM, S1P4 EC50>50 μM, and S1P5 EC50>25 μM. CYM-5541 also shows selectivity over a large panel of protein targets, with no significant activities, in the Ricerca profiling panel of 55 GPCRs, ion channels, and transporters. CYM-5541 allowed us to identify an allosteric site where F263 is a key gate-keeper residue for its affinity and efficacy. The novel allosteric hydrophobic pocket may account for the S1P3 selectivity of CYM-5541[1].
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].

Synonyms	CID-17253208, ML249, CYM 5541
Molecular Weight	316.445
Formula	C19H28N2O2
CAS No.	945128-26-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 39 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Jo E, et al. Novel selective allosteric and bitopic ligands for the S1P(3) receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library GPCR Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

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GLPG2938 ONO-7300243 GSK2018682 Ki16198 SLF1081851 PF-543 Ponesimod CYM5442

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CYM-5541 945128-26-7 G蛋白偶联受体 LPL Receptor S1P Receptor CYM5541 inhibit ML-249 ML249 CYM 5541 ML 249 CID-17253208 Inhibitor Lysophospholipid Receptor inhibitor

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