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 |
|---|---|---|---|
| S7176 |
SKI IISKI II是一种高度选择性的，非ATP竞争性的sphingosine kinase (SphK)抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。 |
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 是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，Ki为3.6 nM。PF-543 可诱导细胞凋亡、坏死和自噬。 |
(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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| S7174 |
Opaganib (ABC294640)Opaganib (ABC294640)是一种口服生物可利用的选择性sphingosine kinase-2 (SphK2)抑制剂，IC50约为 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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| S7791New |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA)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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| S6512 |
Defensamide (MHP)Defensamide (MHP)是sphingosine kinase (SPHK1)激活剂。它可通过增强SPHK1活性、诱导cAMP生成来调节表皮免疫反应。 |
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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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| S6552New |
CYM5541CYM5541是一种选择性的S1P3变构受体激动剂，EC50为72-132 nM。 |
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| S5950 |
FingolimodFingolimod是S1PR调节剂，用于治疗缓解型多发性硬化症。 |
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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。 |
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| S7179 |
Siponimod (BAF312)BAF312 (Siponimod)是一种二代S1P受体调节剂，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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| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7176 |
SKI IISKI II是一种高度选择性的，非ATP竞争性的sphingosine kinase (SphK)抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。 |
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 是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，Ki为3.6 nM。PF-543 可诱导细胞凋亡、坏死和自噬。 |
(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。 |
||
| S7174 |
Opaganib (ABC294640)Opaganib (ABC294640)是一种口服生物可利用的选择性sphingosine kinase-2 (SphK2)抑制剂，IC50约为 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).
|
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7791New |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA)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)。 |
||
| S6512 |
Defensamide (MHP)Defensamide (MHP)是sphingosine kinase (SPHK1)激活剂。它可通过增强SPHK1活性、诱导cAMP生成来调节表皮免疫反应。 |
| 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). |
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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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6552New |
CYM5541CYM5541是一种选择性的S1P3变构受体激动剂，EC50为72-132 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5950 |
FingolimodFingolimod是S1PR调节剂，用于治疗缓解型多发性硬化症。 |
||
| 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。 |
||
| S7179 |
Siponimod (BAF312)BAF312 (Siponimod)是一种二代S1P受体调节剂，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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