S1P Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

S1P Receptor Products

Catalog No. Information Product Use Citations Product Validations
S0817New

SKI-V

SKI-V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase (SPHK/SK) 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 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).

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).

S5002

Fingolimod (FTY720) HCl

Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.

S7182

JTE 013

JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.

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.

S5950

Fingolimod

Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.

S2878New

CYM-5442

CYM-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

Ponesimod

Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

S7180

SEW 2871

SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 nM.

Catalog No. Information Product Use Citations Product Validations
S0817New

SKI-V

SKI-V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase (SPHK/SK) 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 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).

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) HCl

Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.

S7182

JTE 013

JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
S5950

Fingolimod

Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.

S2878New

CYM-5442

CYM-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

Ponesimod

Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

S7180

SEW 2871

SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 nM.