S1P Receptor
Inhibitory Selectivity
Isoform-specific Inhibitors
S1P Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| E0482New |
MP-A08MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2. |
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| 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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| E1123New |
K145K145 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. |
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| 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). |
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| E2363New |
APD334APD334 (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. |
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| E1158New |
CAY10444CAY10444 (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. |
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| 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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| S4462 |
CYM-5520CYM-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. |
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| S3412 |
CYM50308CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM. |
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| S2878 |
CYM-5442CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| E0482New |
MP-A08MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2. |
||
| 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. |
||
| E1123New |
K145K145 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 |
APD334APD334 (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 |
CAY10444CAY10444 (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 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. |
||
| S4462 |
CYM-5520CYM-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 |
CYM50308CYM50308 (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-5442CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM. |
