S1P Receptor
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
S1P Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S0817 |
SKI-VSKI 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. |
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| S6418 |
PF 429242PF 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). |
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| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P). |
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| S5002 |
Fingolimod (FTY720) HClFingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. |
Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. Id-specific TCR-transgenic and nontransgenic SCID mice were inoculated subcutaneously with 105 MOPC315 myeloma cells embedded in Matrigel.9 TCR-transgenic SCID mice were treated daily with fingolimod (1ug/g bodyweight) or with vehicle only (n=8-10). SCID mice were left untreated (n =2). At day 8, draining lymph nodes and Matrigel plugs were dissected and analyzed by flow cytometry.9 (D) CD69 expression on gated Id-specific CD4 T cells in draining lymph nodes of representative TCR-transgenic SCID mice treated with vehicle only (top) or fingolimod (bottom). Dotted lines indicate an isotype-matched control antibody. (E) Number of Id-specific T cells per Matrigel plug (mean SEM). (F) Expression of the activation marker MHC class II on Matrigel-infiltrating CD11b macrophages (geometric mean SEM). P values were calculated with the log-rank test (A-C) and the t test (E-F). ns indicates not significant. |
|
| S7182 |
JTE 013JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
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| S6552 |
CYM5541CYM5541 (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. |
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| 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. |
Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.
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| S5950 |
FingolimodFingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. |
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| S2878New |
CYM-5442CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM. |
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| S7952 |
Ozanimod (RPC1063)Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3. |
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| S8241 |
PonesimodPonesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM. |
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| S7180 |
SEW 2871SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 nM. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S0817 |
SKI-VSKI 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. |
||
| S6418 |
PF 429242PF 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). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5002 |
Fingolimod (FTY720) HClFingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. |
Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. Id-specific TCR-transgenic and nontransgenic SCID mice were inoculated subcutaneously with 105 MOPC315 myeloma cells embedded in Matrigel.9 TCR-transgenic SCID mice were treated daily with fingolimod (1ug/g bodyweight) or with vehicle only (n=8-10). SCID mice were left untreated (n =2). At day 8, draining lymph nodes and Matrigel plugs were dissected and analyzed by flow cytometry.9 (D) CD69 expression on gated Id-specific CD4 T cells in draining lymph nodes of representative TCR-transgenic SCID mice treated with vehicle only (top) or fingolimod (bottom). Dotted lines indicate an isotype-matched control antibody. (E) Number of Id-specific T cells per Matrigel plug (mean SEM). (F) Expression of the activation marker MHC class II on Matrigel-infiltrating CD11b macrophages (geometric mean SEM). P values were calculated with the log-rank test (A-C) and the t test (E-F). ns indicates not significant. |
|
| S7182 |
JTE 013JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6552 |
CYM5541CYM5541 (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. |
Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5950 |
FingolimodFingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. |
||
| S2878New |
CYM-5442CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM. |
||
| S7952 |
Ozanimod (RPC1063)Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3. |
||
| S8241 |
PonesimodPonesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM. |
||
| S7180 |
SEW 2871SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 nM. |
