CYM-5478

Description

CYM 5478 is a sphingosine-1-phosphate receptor 2 (S1P₂) agonist (EC₅₀ = 0.78 μM in a reporter assay). It is selective for S1P₂ over S1P₁ and S1P_3-5 in a TGFα-shedding assay (EC₅₀s = 119, 1,690, 1,950, >10,000, and >10,000 nM, respectively). CYM 5478 (0.1-10 μM) reduces serum starvation-induced decreases in C6 rat glioma cell viability. It also reduces accumulation of reactive oxygen species (ROS) and apoptosis induced by cisplatin in C6 cells when used at a concentration of 10 μM.

Uses

CYM-5478 is a potent and highly selective S1P2 agonist with an EC50 of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity[1][2].

in vivo

IC 50

S1PR2: 119 nM (EC₅₀); S1PR1: 1690 nM (EC₅₀); S1PR3: 1950 nM (EC₅₀); S1PR4: >10 μM (EC₅₀); S1PR5: >10 μM (IC₅₀)

References

[1] Deron R Herr, et al. Sphingosine 1-phosphate receptor 2 (S1P2) attenuates reactive oxygen species formation and inhibits cell death: implications for otoprotective therapy. Sci Rep. 2016 Apr 15;6:24541. DOI:10.1038/srep24541
[2] Wei Wang, et al. Sphingosine 1-Phosphate Receptor 2 Induces Otoprotective Responses to Cisplatin Treatment. Cancers (Basel). 2020 Jan 15;12(1):211. DOI:10.3390/cancers12010211