Product Details
| Product Name:
CYM-5541 |
CAS No.:
945128-26-7 |
| Purity:
98.39% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (158.01 mM)
|
| Keywords | inhibit | LPL Receptor | CID 17253208 | ML-249 | CID17253208 | CYM-5541 | Inhibitor | Lysophospholipid Receptor | CYM5541 | ML 249 |
| Inhibitors Related | Fingolimod hydrochloride | SLP9101555 | SKI-178 | LX-2931 | Tyloxapol | ASP-4058 | Ki16198 | Siponimod | Fingolimod | MP-A08 | S1PR1 modulator 1 | Ozanimod |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States