S5002 |
Fingolimod (FTY720) HCl
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Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.Please use saline solution rather than PBS for dilutions. PBS may cause precipitation. |
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J Exp Med, 2024, 221(4)e20232104
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Cell Rep Med, 2024, S2666-3791(24)00544-5
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Cell Death Dis, 2024, 15(9):678
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S7791 |
PMA (Phorbol 12-myristate 13-acetate)
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PMA (Phorbol 12-myristate 13-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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Cell Rep Med, 2024, 5(8):101686
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J Exp Clin Cancer Res, 2024, 43(1):105
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Cell Mol Biol Lett, 2024, 29(1):77
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S5950 |
Fingolimod (FTY-720)
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Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. |
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Nat Commun, 2024, 15(1):6970
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Oncol Res, 2023, 31(6):867-875
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J Clin Invest, 2022, 132(3)e153604
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S7179 |
Siponimod (BAF312)
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BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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. |
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Cancers (Basel), 2024, 16(3)574
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J Neuroinflammation, 2023, 20(1):35
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Cell Res, 2022, 10.1038/s41422-022-00614-0
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S7182 |
JTE 013
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JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
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Front Pharmacol, 2024, 15:1494210
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Cell Res, 2022, 10.1038/s41422-022-00614-0
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Autophagy, 2022, 1-20
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S7952 |
Ozanimod
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Ozanimod is a selective oral S1P Receptor 1 modulator. Phase 3.
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Front Immunol, 2024, 15:1230735
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FASEB J, 2022, 36(2):e22132
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China Biotechnology, 2020, (6): 10-19
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S8241 |
Ponesimod
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Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM. |
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Cancers (Basel), 2024, 16(3)574
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EBioMedicine, 2023, 94:104713
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Int J Mol Sci, 2022, 23(18)10311
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S6418 |
PF 429242
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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). |
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Cell Rep, 2023, 42(6):112586
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Nat Commun, 2019, 11;10(1):4621
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S0817 |
SKI-V
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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. |
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Cell Death Discov, 2022, 8(1):48
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Cell Death Discov, 2022, 8(1):48
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E2363New |
Etrasimod(APD334)
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Etrasimod(APD334) 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. |
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E0482 |
MP-A08
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MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2. |
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E1917New |
SLF1081851 hydrochloride
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SLF1081851 hydrochloride is a potential inhibitor of Spns2 that blocks S1P release with an IC50 of 1.93 μM. It can be developed as a probe for studying Spns2 biology and immune modulation. |
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E1218 |
K6PC-5
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K6PC-5, a ceramide derivative, is a sphingosine kinase 1 (SPHK1) activator and elicits a rapid transient increase in intracellular calcium levels. |
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Cell Prolif, 2024, e13604.
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Int J Biol Sci, 2022, 18(7):2994-3005
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E1123 |
K145
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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. |
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E1158 |
CAY10444
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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. |
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S6552 |
CYM5541
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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. |
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S4462 |
CYM-5520
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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. |
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Front Pharmacol, 2024, 15:1494210
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S3412 |
CYM50308
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CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM. |
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E4956New |
Ozanimod hydrochloride
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Ozanimod hydrochloride(Zeposia, RPC-1063 HCL) is a potent sphingosine 1-phosphate (S1P)receptor modulator and a selective agonist of S1P receptor subtypes 1 (S1P1) and 5 (S1P5) with EC50's of 1.03 nM and 8.6 nM, respectively. It can be used in the trearment of relapsing multiple sclerosis (MS). |
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E2411 |
Taurodeoxycholic acid sodium hydrate
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Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. It activates S1PR2 pathway in addition to the TGR5 pathway. |
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S7179 |
Siponimod (BAF312)
|
BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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. |
-
Cancers (Basel), 2024, 16(3)574
-
J Neuroinflammation, 2023, 20(1):35
-
Cell Res, 2022, 10.1038/s41422-022-00614-0
|
|
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. |
|
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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. |
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Front Pharmacol, 2024, 15:1494210
|
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S3412 |
CYM50308
|
CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM. |
|
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E4956New |
Ozanimod hydrochloride
|
Ozanimod hydrochloride(Zeposia, RPC-1063 HCL) is a potent sphingosine 1-phosphate (S1P)receptor modulator and a selective agonist of S1P receptor subtypes 1 (S1P1) and 5 (S1P5) with EC50's of 1.03 nM and 8.6 nM, respectively. It can be used in the trearment of relapsing multiple sclerosis (MS). |
|
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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). |
- Cell Rep, 2023, 42(6):112586
- Nat Commun, 2019, 11;10(1):4621
|
|
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
- Cell Death Discov, 2022, 8(1):48
|
|
E0482 |
MP-A08
|
MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2. |
|
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E1917New |
SLF1081851 hydrochloride
|
SLF1081851 hydrochloride is a potential inhibitor of Spns2 that blocks S1P release with an IC50 of 1.93 μM. It can be developed as a probe for studying Spns2 biology and immune modulation. |
|
|
E1123 |
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. |
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