S1P Receptor
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
S1P Receptor产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0817New |
SKI-VSKI-V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase (SPHK/SK) 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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| S6418 |
PF 429242PF 429242是S1P抑制剂，IC50为170 nM。在其浓度高达100 μM时，PF 429242对胰蛋白酶、弹性蛋白酶、蛋白酶K、胞浆素、激肽释放酶、factor XIa、凝血酶或弗林蛋白酶没有显著抑制作用，而对尿激酶和factor Xa仅具有中等抑制作用。 |
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| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA, 12-O-Tetradecanoylphorbol-13-acetate, TPA)是一种有效的PKC激活剂，在纳摩尔浓度范围内具有活性作用。Phorbol 12-myristate 13-acetate (PMA)可诱导sphingosine-1-phosphate (S1P)。 |
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| S5002 |
Fingolimod (FTY720) HClFingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。 |
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是sphingosine 1-phosphate receptor 2(S1P2)拮抗剂（IC50=17.6 nM）。在超过10 μM的浓度下，对S1P1或S1P3没有作用。在HTC4细胞中，JTE-013拮抗S1P4的Ki值为237 nM。 |
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| S6552 |
CYM5541CYM5541 (ML249)是一种选择性的S1P3变构受体激动剂，EC50为72-132 nM。 |
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| S7179 |
Siponimod (BAF312)BAF312 (Siponimod)是一种二代S1P受体激动剂，选择性作用于S1P1和S1P5受体，EC50分别为0.39 nM和0.98 nM，比作用于S1P2， S1P3和S1P4受体选择性高1000倍以上。 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)是S1PR调节剂，用于治疗缓解型多发性硬化症。 |
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| S2878New |
CYM-5442CYM-5442是一种强有效和选择性的S1P1激动剂，EC50为1.35 nM。 |
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| S7180New |
SEW 2871SEW 2871是一种选择性的S1P1受体激动剂，EC50为13 nM。 |
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| S7952 |
Ozanimod (RPC1063)Ozanimod (RPC1063)是一种选择性口服的 S1P Receptor 1 调节剂。Phase 3。 |
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| S8241 |
PonesimodPonesimod (ACT-128800)是一种具有口服活性的S1P1免疫调制剂，其EC50为5.7 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0817New |
SKI-VSKI-V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase (SPHK/SK) 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. |
||
| S6418 |
PF 429242PF 429242是S1P抑制剂，IC50为170 nM。在其浓度高达100 μM时，PF 429242对胰蛋白酶、弹性蛋白酶、蛋白酶K、胞浆素、激肽释放酶、factor XIa、凝血酶或弗林蛋白酶没有显著抑制作用，而对尿激酶和factor Xa仅具有中等抑制作用。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA, 12-O-Tetradecanoylphorbol-13-acetate, TPA)是一种有效的PKC激活剂，在纳摩尔浓度范围内具有活性作用。Phorbol 12-myristate 13-acetate (PMA)可诱导sphingosine-1-phosphate (S1P)。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5002 |
Fingolimod (FTY720) HClFingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。 |
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是sphingosine 1-phosphate receptor 2(S1P2)拮抗剂（IC50=17.6 nM）。在超过10 μM的浓度下，对S1P1或S1P3没有作用。在HTC4细胞中，JTE-013拮抗S1P4的Ki值为237 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6552 |
CYM5541CYM5541 (ML249)是一种选择性的S1P3变构受体激动剂，EC50为72-132 nM。 |
||
| S7179 |
Siponimod (BAF312)BAF312 (Siponimod)是一种二代S1P受体激动剂，选择性作用于S1P1和S1P5受体，EC50分别为0.39 nM和0.98 nM，比作用于S1P2， S1P3和S1P4受体选择性高1000倍以上。 Phase 3。 |
Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.
|
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5950 |
FingolimodFingolimod (FTY-720A, FTY-720)是S1PR调节剂，用于治疗缓解型多发性硬化症。 |
||
| S2878New |
CYM-5442CYM-5442是一种强有效和选择性的S1P1激动剂，EC50为1.35 nM。 |
||
| S7180New |
SEW 2871SEW 2871是一种选择性的S1P1受体激动剂，EC50为13 nM。 |
||
| S7952 |
Ozanimod (RPC1063)Ozanimod (RPC1063)是一种选择性口服的 S1P Receptor 1 调节剂。Phase 3。 |
||
| S8241 |
PonesimodPonesimod (ACT-128800)是一种具有口服活性的S1P1免疫调制剂，其EC50为5.7 nM。 |
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