S1P Receptor
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
S1P Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7176 |
SKI IISKI II is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2. |
Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.
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| S7177 |
PF-543PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy. |
(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; *P < 0.05, **P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
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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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| S7174 |
Opaganib (ABC294640)Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2. |
Macrophages treated with ABC294640 at concentrations of 0, 0.5, 1, 5, 10, 50, or 100 nM. Ratios of OD/OD (NC) are presented as means ± standard deviation. *p < 0.05 vs. NC group (1‰ DMSO).
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| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA), 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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| S6512 |
Defensamide (MHP)Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production. |
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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. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6 105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8). |
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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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| 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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| S7181New |
W146W146 is a potent S1P1 selective antagonist with Ki of 18 nM. |
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| S7180New |
SEW 2871SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7176 |
SKI IISKI II is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2. |
Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.
|
|
| S7177 |
PF-543PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy. |
(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; *P < 0.05, **P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
|
|
| 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). |
||
| S7174 |
Opaganib (ABC294640)Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2. |
Macrophages treated with ABC294640 at concentrations of 0, 0.5, 1, 5, 10, 50, or 100 nM. Ratios of OD/OD (NC) are presented as means ± standard deviation. *p < 0.05 vs. NC group (1‰ DMSO).
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P). |
||
| S6512 |
Defensamide (MHP)Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production. |
| 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. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6 105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8). |
|
| 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. |
||
| S7181New |
W146W146 is a potent S1P1 selective antagonist with Ki of 18 nM. |
||
| S7180New |
SEW 2871SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 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. |
