S1P Receptor

Inhibitory Selectivity

Isoform-specific Inhibitors

S1P Receptor Products

New S1P Receptor Products
Catalog No. 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.

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.

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.

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).

E2363New

APD334

APD334 (Etrasimod ) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

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.

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.

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.

S2878

CYM-5442

CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM.

Catalog No. 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.

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.

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.

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, Phorbol myristate acetate), 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
E2363New

APD334

APD334 (Etrasimod ) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S2878

CYM-5442

CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM.