S1P Receptor

Isoform-selective Products

Signaling Pathway

S1P Receptor Signaling Pathway

S1P Receptor Products

  • All (18)
  • S1P Receptor Inhibitors (4)
  • S1P Receptor Activators (3)
  • S1P Receptor Antagonists (4)
  • S1P Receptor Agonists (4)
  • S1P Receptor Modulators (3)
  • New S1P Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S5002 Fingolimod (FTY720) HCl 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.
J Exp Med, 2024, 221(4)e20232104
Cell, 2023, 10.1016/j.cell.2023.10.022
Nat Commun, 2023, 14(1):7709.
S7791 PMA (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.
Cancer Commun (Lond), 2023, 43(8):909-937
Cell Rep, 2023, 42(8):112944
Elife, 2023, 12e85494
S5950 Fingolimod (FTY-720) Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
Oncol Res, 2023, 31(6):867-875
J Clin Invest, 2022, 132(3)e153604
J Clin Invest, 2022, 132(3)e153604
S7179 Siponimod (BAF312) BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.
Cancers (Basel), 2024, 16(3)574
J Neuroinflammation, 2023, 20(1):35
Cell Res, 2022, 10.1038/s41422-022-00614-0
S7182 JTE 013 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Autophagy, 2022, 1-20
Vascul Pharmacol, 2021, S1537-1891(21)00113-0
S7952 Ozanimod Ozanimod is a selective oral S1P Receptor 1 modulator. Phase 3.
FASEB J, 2022, 36(2):e22132
China Biotechnology, 2020, (6): 10-19
Nucleic Acids Res, 2019, 10.1093/nar/gkz1136
S8241 Ponesimod 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
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
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
Cell Death Discov, 2022, 8(1):48
E2363New Etrasimod(APD334) Etrasimod(APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an EC50 value of 1.88 nM in CHO cells.
E0482 MP-A08 MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2.
E1218 K6PC-5 K6PC-5, a ceramide derivative, is a sphingosine kinase 1 (SPHK1) activator and elicits a rapid transient increase in intracellular calcium levels.
Cell Prolif, 2024, e13604.
E1123 K145 K145 is a selective, substrate-competitive and orally active sphingosine kinase-2 (SphK2) inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM in biochemical assays.
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.
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.
S4462 CYM-5520 CYM-5520 is a highly selective sphingosine-1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 0.48 µM and does not activate other S1P receptors.
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
E2411 Taurodeoxycholic acid sodium hydrate Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. It activates S1PR2 pathway in addition to the TGR5 pathway.
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
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
Cell Death Discov, 2022, 8(1):48
E0482 MP-A08 MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2.
E1123 K145 K145 is a selective, substrate-competitive and orally active sphingosine kinase-2 (SphK2) inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM in biochemical assays.
S7791 PMA (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.
Cancer Commun (Lond), 2023, 43(8):909-937
Cell Rep, 2023, 42(8):112944
Elife, 2023, 12e85494
E1218 K6PC-5 K6PC-5, a ceramide derivative, is a sphingosine kinase 1 (SPHK1) activator and elicits a rapid transient increase in intracellular calcium levels.
Cell Prolif, 2024, e13604.
E2411 Taurodeoxycholic acid sodium hydrate Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. It activates S1PR2 pathway in addition to the TGR5 pathway.
S5002 Fingolimod (FTY720) HCl 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.
J Exp Med, 2024, 221(4)e20232104
Cell, 2023, 10.1016/j.cell.2023.10.022
Nat Commun, 2023, 14(1):7709.
S7182 JTE 013 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Autophagy, 2022, 1-20
Vascul Pharmacol, 2021, S1537-1891(21)00113-0
E2363New Etrasimod(APD334) Etrasimod(APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an EC50 value of 1.88 nM in CHO cells.
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.
S7179 Siponimod (BAF312) BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.
Cancers (Basel), 2024, 16(3)574
J Neuroinflammation, 2023, 20(1):35
Cell Res, 2022, 10.1038/s41422-022-00614-0
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.
S4462 CYM-5520 CYM-5520 is a highly selective sphingosine-1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 0.48 µM and does not activate other S1P receptors.
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
S5950 Fingolimod (FTY-720) Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
Oncol Res, 2023, 31(6):867-875
J Clin Invest, 2022, 132(3)e153604
J Clin Invest, 2022, 132(3)e153604
S7952 Ozanimod Ozanimod is a selective oral S1P Receptor 1 modulator. Phase 3.
FASEB J, 2022, 36(2):e22132
China Biotechnology, 2020, (6): 10-19
Nucleic Acids Res, 2019, 10.1093/nar/gkz1136
S8241 Ponesimod 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
E2363New Etrasimod(APD334) Etrasimod(APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an EC50 value of 1.88 nM in CHO cells.

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