Home GPCR & G Protein S1P Receptor

S1P Receptor modulators/antagonists

Sphingosine 1-phosphate receptors are G-protein-coupling receptors which contain 5 members called S1P1, S1P2, S1P3, S1P4, S1P5 receptors. The activation of S1P receptors can result in activation of the small guanosine triphosphatase (GTPase) Ras and the extracellular signal-regulated kinase (ERK) leading to proliferation. Signaling started from S1P receptor is associated with activation of phosphatidylinositol 3-kinase (PI3-K) and protein kinase B (PKB or Akt) which are involved in increasing survival or inhibiting apoptosis. Activation of protein kinase C (PKC) and phospholipase C (PLC) are also related to S1P receptors leading to increasing free calcium in cell.

Other GPCR & G Protein Related Inhibitors

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S5002 FTY720 (Fingolimod) Hydrochloride Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.
Cancer Cell, 2025, S1535-6108(25)00319-8
Nat Commun, 2025, 16(1):9175
Nat Commun, 2025, 16(1):1826
Verified customer review of FTY720 (Fingolimod) Hydrochloride
S7791 PMA chemical (Phorbol 12-myristate 13-acetate) PMA (Phorbol 12-myristate 13-acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).PMA has strong excitability on the skin and mucous membrane. Special protection is required when using PMA. Wear gloves and mask to avoid direct contact in any way.
Protein Cell, 2025, pwaf020
Nat Commun, 2025, 16(1):8054
Cancer Commun (Lond), 2025, 10.1002/cac2.70036
S5950 Fingolimod (FTY-720) Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
Nat Commun, 2024, 15(1):6970
Ther Adv Neurol Diso, 2024, 17:17562864241300047
Oncol Res, 2023, 31(6):867-875
S7179 Siponimod (BAF312) Siponimod (BAF312) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, and it exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. This compound has reached Phase 3.
Cell Death Dis, 2025, 16(1):282
Cancers (Basel), 2024, 16(3)574
J Neuroinflammation, 2023, 20(1):35
Verified customer review of Siponimod (BAF312)
S7182 JTE 013 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
Cell Death Dis, 2025, 16(1):282
PLoS ONE, 2025, e0317568
Front Pharmacol, 2024, 15:1494210
S7952 Ozanimod Ozanimod is a selective oral S1P Receptor 1 modulator. Phase 3.
Nat Commun, 2025, 16(1):1826
Front Immunol, 2024, 15:1230735
Frontiers in Pharmacology, 2022, 892097
S8241 Ponesimod (ACT-128800) Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
Cancers (Basel), 2024, 16(3)574
EBioMedicine, 2023, 94:104713
Int J Mol Sci, 2022, 23(18)10311
E1158 CAY10444 CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist, which can inhibit S1P response of S1P3 cell line with 78% inhibition rate and IC50 of 4.6 μM.
Cell Death Dis, 2025, 16(1):282
J Transl Med, 2025, 23(1):573
S6418 PF 429242 PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).
Cell Rep, 2023, 42(6):112586
Nat Commun, 2019, 11;10(1):4621
S6552 CYM5541 CYM5541 (ML249) is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM.
Brain Behav Immun, 2024, 124:205-217

Signaling Pathway Map