S1P Receptor
S1P Receptor产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S0817 |
SKI-VSKI V是一种非竞争性且有效的非脂质sphingosine kinase抑制剂,对GST-hSK的IC50为 2 μM。SKI-V 还抑制 PI3K,对hPI3k的 IC50 为 6 μM。SKI-V 减少促有丝分裂第二信使sphingosine-1-phosphate(S1P)的形成,并通过抗肿瘤活性诱导细胞凋亡。 |
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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, Phorbol myristate acetate)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。 |
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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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S4462 |
CYM-5520CYM-5520 是一种高选择性 1-磷酸鞘氨醇受体 2 (sphingosine-1-phosphate receptor 2,S1PR2) 激动剂,EC50 为 0.48 µM,不会激活其他 S1P 受体。 |
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S3412 |
CYM50308CYM50308 (ML248) 是一种有效的选择性 S1P4 受体激动剂,EC50 为 56 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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S2878 |
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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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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S7180 |
SEW 2871SEW 2871是一种选择性的S1P1受体激动剂,EC50为13 nM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S0817 |
SKI-VSKI V是一种非竞争性且有效的非脂质sphingosine kinase抑制剂,对GST-hSK的IC50为 2 μM。SKI-V 还抑制 PI3K,对hPI3k的 IC50 为 6 μM。SKI-V 减少促有丝分裂第二信使sphingosine-1-phosphate(S1P)的形成,并通过抗肿瘤活性诱导细胞凋亡。 |
||
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, Phorbol myristate acetate)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). |
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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 |
---|---|---|---|
S6552 |
CYM5541CYM5541 (ML249)是一种选择性的S1P3变构受体激动剂,EC50为72-132 nM。 |
||
S4462 |
CYM-5520CYM-5520 是一种高选择性 1-磷酸鞘氨醇受体 2 (sphingosine-1-phosphate receptor 2,S1PR2) 激动剂,EC50 为 0.48 µM,不会激活其他 S1P 受体。 |
||
S3412 |
CYM50308CYM50308 (ML248) 是一种有效的选择性 S1P4 受体激动剂,EC50 为 56 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。 |
||
S2878 |
CYM-5442CYM-5442是一种强有效和选择性的S1P1激动剂,EC50为1.35 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。 |
||
S7180 |
SEW 2871SEW 2871是一种选择性的S1P1受体激动剂,EC50为13 nM。 |