S1P Receptor

Choose Selective S1P Receptor Inhibitors

S1P Receptor Signaling Pathway Map

S1P Receptor Signaling Pathways

S1P Receptor Products

  • All (17)
  • S1P Receptor Inhibitors (4)
  • S1P Receptor Activator (1)
  • S1P Receptor Antagonists (4)
  • S1P Receptor Agonists (4)
  • S1P Receptor Modulators (4)
  • New S1P Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0482New MP-A08 MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2.
E1123New 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.
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
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).
Nat Commun, 2019, 11;10(1):4621
S7791 Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
Oncogene, 2022, 10.1038/s41388-022-02197-x
Sci Rep, 2022, 12(1):1626
E1158New 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.
E2363New APD334 APD334 (Etrasimod ) 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.
S5002 Fingolimod (FTY720) HCl Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.
Cancer Cell, 2022, S1535-6108(22)00004-6
J Clin Invest, 2022, 132(3)e153604
J Immunother Cancer, 2022, 10(5)e003960
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
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
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.
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.
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.
Cell Res, 2022, 10.1038/s41422-022-00614-0
FASEB J, 2022, 36(2):e22132
J Nanobiotechnology, 2021, 19(1):165
S2878 CYM-5442 CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM.
Antiviral Res, 2020, S0166-3542(20)30413-7
S5950 Fingolimod Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
J Clin Invest, 2022, 132(3)e153604
J Immunother Cancer, 2022, 10(5)e003960
Clin Transl Med, 2022, 12(2):e695
S7952 Ozanimod (RPC1063) Ozanimod (RPC1063) 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.
Antiviral Res, 2020, S0166-3542(20)30413-7
FEBS Open Bio, 2020, 10.1002/2211-5463.12951
Leukemia, 2019, 10.1038/s41375-019-0478-9
E0482New MP-A08 MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2.
E1123New 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.
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
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).
Nat Commun, 2019, 11;10(1):4621
S7791 Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
Oncogene, 2022, 10.1038/s41388-022-02197-x
Sci Rep, 2022, 12(1):1626
E1158New 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.
E2363New APD334 APD334 (Etrasimod ) 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.
S5002 Fingolimod (FTY720) HCl Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.
Cancer Cell, 2022, S1535-6108(22)00004-6
J Clin Invest, 2022, 132(3)e153604
J Immunother Cancer, 2022, 10(5)e003960
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
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
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.
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.
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.
Cell Res, 2022, 10.1038/s41422-022-00614-0
FASEB J, 2022, 36(2):e22132
J Nanobiotechnology, 2021, 19(1):165
S2878 CYM-5442 CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM.
Antiviral Res, 2020, S0166-3542(20)30413-7
S5950 Fingolimod Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
J Clin Invest, 2022, 132(3)e153604
J Immunother Cancer, 2022, 10(5)e003960
Clin Transl Med, 2022, 12(2):e695
S7952 Ozanimod (RPC1063) Ozanimod (RPC1063) 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.
Antiviral Res, 2020, S0166-3542(20)30413-7
FEBS Open Bio, 2020, 10.1002/2211-5463.12951
Leukemia, 2019, 10.1038/s41375-019-0478-9
E0482New MP-A08 MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2.
E1123New 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.
E1158New 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.
E2363New APD334 APD334 (Etrasimod ) 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.
Tags: S1P Receptor inhibitor|S1P Receptor agonist|S1P Receptor activator|S1P Receptor inducer|S1P Receptor antagonist|S1P Receptor signaling pathway|S1P Receptor assay kit