S1P Receptor
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S7176 | SKI II | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S7177 | PF-543 | <1 mg/mL | 93 mg/mL | 93 mg/mL |
| S7174 | Opaganib (ABC294640) | <1 mg/mL | 76 mg/mL | 28 mg/mL |
| S5002 | Fingolimod (FTY720) HCl | 69 mg/mL | 69 mg/mL | 69 mg/mL |
| S7182 | JTE 013 | <1 mg/mL | 81 mg/mL | 34 mg/mL |
| S5950 | Fingolimod | <1 mg/mL | 13 mg/mL | 5 mg/mL |
| S7952 | Ozanimod (RPC1063) | <1 mg/mL | 81 mg/mL | 10 mg/mL |
| S8241 | Ponesimod | <1 mg/mL | 92 mg/mL | 92 mg/mL |
| S7179 | Siponimod (BAF312) | <1 mg/mL | 100 mg/mL | 44 mg/mL |
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. |
D, representative merged IF images with DAPI nuclei staining (blue) in untreated (“Ctl”) and CoCl2-treated cells without (“Veh”), and with SKI-II co-treatment. Scale bar = 30 μm. N=5 independent samples per group. oligodendrocytes(defined by MBP immunoreactivity, red), oligodendrocyte progenitor cell(defined by NG2 immunoreactivity, green).
|
|
| 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. |
(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).
|
|
| 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).
|
|
| 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. |
||
| S5950New |
FingolimodFingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. |
||
| 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. |
||
| 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. |
Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.
|
| 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. |
D, representative merged IF images with DAPI nuclei staining (blue) in untreated (“Ctl”) and CoCl2-treated cells without (“Veh”), and with SKI-II co-treatment. Scale bar = 30 μm. N=5 independent samples per group. oligodendrocytes(defined by MBP immunoreactivity, red), oligodendrocyte progenitor cell(defined by NG2 immunoreactivity, green).
|
|
| 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. |
(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).
|
|
| 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 |
|---|---|---|---|
| S5002 |
Fingolimod (FTY720) HClFingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. |
2012, 119(9):2176-7 2014, 76(3):325-37 2015, 29(4):847-57 |
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 |
|---|---|---|---|
| S5950New |
FingolimodFingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. |
||
| 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. |
||
| 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. |
2018, 32(1):214-223 |
Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.
|
