Syk
信号通路图
研究领域
抑制剂选择性比较
Syk产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2194 |
R406R406 是一种有效的 Syk 抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。R406 可诱导凋亡。Phase 1。 |
Platelets (3 x 108/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).
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| S2206 |
Fostamatinib (R788) disodiumFostamatinib disodium (R788, Tamatinib Fosdium)是活性代谢物R406的前体药物，是一种Syk抑制剂，无细胞试验中IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果弱5倍。Phase 3。 |
BCWM.1 and MWCL-1 cells treated with either vehicle or fostamatinib at the indicated concentrations for two hours, then protein extracts were analyzed by Western blotting for the activation status of MEK, p44/42 MAPK, and Akt with phospho-specific antibodies.
|
|
| S1533 |
R406 (free base)R406 (free base) 是一种有效的Syk抑制剂，无细胞试验中IC50为41 nM，强效抑制Syk而不能抑制Lyn，对Flt3作用效果低5倍。R406 (free base) 可触发凋亡。Phase 1。 |
(C) Z-138 and JEKO-1 cells were simultaneously exposed to sorafenib and R406 at the indicated doses, and cell viability was determined at 48 hours by annexin V/PI staining. Bars represent the mean ± SD of 3 independent experiments. CI value is indicated for each combination. (D) Primary MCL cells from 7 patients were simultaneously exposed to sorafenib and R406 at the indicated doses for 48 hours, and cell viability was determined as above. Bars represent the mean ± SEM of all the samples analyzed. CI value is indicated for each combination. |
|
| S8032 |
PRT062607 (P505-15) HClPRT062607 (P505-15, BIIB057, PRT-2607)是一种新型的，高度选择性Syk抑制剂，无细胞试验中IC50为1 nM，作用于Syk比作用于Fgr，PAK5，Lyn，FAK，Pyk2, FLT3, MLK1 和Zap70选择性高80倍以上。 |
Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.
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| S2625 |
Fostamatinib (R788)Fostamatinib (R788)是活性代谢产物R406的前体药物，是一种Syk抑制剂，IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果低5倍。Phase 3。 |
B cells were stimulated by irradiated CD40L+ L cells. Forward scatter vs. BrdU incorporation analysis (day 5) in the gated CD19+ CLL cells (D). The distribution of cells with high FSC (blasts, right quadrants) and proliferation (BrdU+, upper quadrants) are shown.
|
|
| S3026 |
PiceatannolPiceatannol，是一种天然二苯乙烯，是选择性Syk抑制剂，比作用于Lyn选择性高10倍左右。 |
Change of protein and mRNA with or without the pretreatment of Syk inhibitors. After pretreated with PRT062607 and Piceatannol for 30 min before A. fumigatus hyphae stimulation, activation of Syk was inhibited by 1 μM PRT062607 (p < 0.05), 2 μM PRT062607 (p < 0.01), 5 μM Piceatannol (p < 0.05), 10 μM Piceatannol (p < 0.01) a compared with untreated cells. mRNA expression of IL-1β, IL-6, IL-8 and CXCL1 induced by A. fumigatus hyphae were significantly suppressed b. mRNA expression of IL-1β, IL-6, IL-8, CXCL1 downregulated significantly by 1 μM PRT062607, 2 μM PRT062607, 5 μM Piceatannol, 10 μM Piceatannol. **means p < 0.01, *p < 0.05. |
|
| S4921 |
MNS (3,4-Methylenedioxy-β-nitrostyrene)MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)是一种酪氨酸激酶抑制剂，抑制Syk， Src和p97， IC50分别为2.5 μM， 29.3 μM和1.7 μM。 |
WT mouse primary macrophages were untreated as control (lane 1) or treated with 0.1μg/ml E. coli LPS (lane 5-8), 10μM E-64 (lane 2 and 6), 250μM PMSF (lane 3 and 7), or 20μM MNS (lane 4 and 8). The cells were continuously cultured for 16 hrs. Extracts from whole cells or nuclei were separately purified and subjected to WB analysis with antibody against pERK2, LITAF, or actin/tubulin as control.
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| S7286 |
RO9021RO9021有效地抑制Syk激酶活性，IC50为5.6nM。它还能够抑制B细胞受体信号通路。 |
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| S6519 |
R112R112是ATP竞争性Syk抑制剂，Ki值为96 nM。 |
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| S3226 |
Dehydroabietic acidDehydroabietic acid (DAA, DHAA) 是一种天然的二萜树脂酸，衍生自针叶植物（如 Pinus 和 Picea）通过抑制 Src、Syk 和 TAK1 介导的通路来产生抗炎活性。 |
||
| S4944 |
Fostamatinib disodium hexahydrateFostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate 是活性代谢产物R406的前药，是一种 Syk 的抑制剂，在无细胞分析中的IC50值为41 nM。 |
||
| S0871 |
Gusacitinib (ASN-002)Gusacitinib (ASN-002) 是一种新型有效的脾酪氨酸激酶 (SYK) 和 Janus 激酶 (JAK) 双重抑制剂，在生化试验中 IC50 值为 5-46 nM。 |
||
| S8442 |
TAK-659TAK-659是一种有效的、选择性的SYK抑制剂。IC50为3.2 nM。对其他激酶具有选择性，对FLT3也能有效抑制，IC50为4.6 nM。 |
||
| S7738 |
PRT-060318 2HClPRT-060318 (PRT318) 是一种新型选择性Syk酪氨酸激酶抑制剂，IC50为4 nM。是一种肝素诱导性血小板减少症的治疗方法。 |
||
| S9715 |
Lanraplenib (GS-9876)Lanraplenib (GS-9876, GS-SYK) 是一种有效的、高选择性的 Spleen Tyrosine Kinase (SYK) 的口服活性抑制剂，其IC50值为9.5 nM。Lanraplenib 通过 glycoprotein VI (GPVI) receptor 抑制血小板中的SYK活性，而不会延长猴子或人类的出血时间(BT)。 |
||
| S8948 |
SRX3207SRX3207 是一种口服活性的 Syk-PI3K 的双重抑制剂，对 Syk、Zap70、BRD41、BRD42、PI3K alpha、PI3K delta、PI3K gamma 的IC50值分别为39.9 nM、31200 nM、3070 nM、3070 nM、244 nM、388 nM、9790 nM。SRX3207 会阻断肿瘤免疫抑制并增加抗肿瘤免疫力。 |
||
| S3566 |
Cerdulatinib (PRT062070)Cerdulatinib (PRT-062070, PRT2070) 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
||
| S7634 |
Cerdulatinib (PRT062070) hydrochlorideCerdulatinib (PRT-062070, PRT2070) hydrochloride 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
||
| S7523 |
Entospletinib (GS-9973)Entospletinib (GS-9973)是一种口服具有生物活性的，选择性Syk抑制剂，无细胞试验中IC50为7.7 nM。在细胞中，对Syk的选择性比对其他激酶（如Jak2, ckit, Flt3, Ret, KDR）高13-1000倍。 |
Dose titration effects of sotrastaurin (Sotr), GS-9973 (GS) on GSK-3 and AKT phosphorylation were evaluated in anti-IgM-stimulated CLL cells. One representative experiment out of 3 performed is shown.
|
|
| S7006 |
BAY-61-3606BAY-61-3606是一种有效的、选择性的Syk激酶抑制剂，Ki为7.5 nM。BAY-61-3606可诱导细胞周期阻滞和凋亡。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2194 |
R406R406 是一种有效的 Syk 抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。R406 可诱导凋亡。Phase 1。 |
Platelets (3 x 108/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).
|
|
| S2206 |
Fostamatinib (R788) disodiumFostamatinib disodium (R788, Tamatinib Fosdium)是活性代谢物R406的前体药物，是一种Syk抑制剂，无细胞试验中IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果弱5倍。Phase 3。 |
BCWM.1 and MWCL-1 cells treated with either vehicle or fostamatinib at the indicated concentrations for two hours, then protein extracts were analyzed by Western blotting for the activation status of MEK, p44/42 MAPK, and Akt with phospho-specific antibodies.
|
|
| S1533 |
R406 (free base)R406 (free base) 是一种有效的Syk抑制剂，无细胞试验中IC50为41 nM，强效抑制Syk而不能抑制Lyn，对Flt3作用效果低5倍。R406 (free base) 可触发凋亡。Phase 1。 |
(C) Z-138 and JEKO-1 cells were simultaneously exposed to sorafenib and R406 at the indicated doses, and cell viability was determined at 48 hours by annexin V/PI staining. Bars represent the mean ± SD of 3 independent experiments. CI value is indicated for each combination. (D) Primary MCL cells from 7 patients were simultaneously exposed to sorafenib and R406 at the indicated doses for 48 hours, and cell viability was determined as above. Bars represent the mean ± SEM of all the samples analyzed. CI value is indicated for each combination. |
|
| S8032 |
PRT062607 (P505-15) HClPRT062607 (P505-15, BIIB057, PRT-2607)是一种新型的，高度选择性Syk抑制剂，无细胞试验中IC50为1 nM，作用于Syk比作用于Fgr，PAK5，Lyn，FAK，Pyk2, FLT3, MLK1 和Zap70选择性高80倍以上。 |
Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.
|
|
| S2625 |
Fostamatinib (R788)Fostamatinib (R788)是活性代谢产物R406的前体药物，是一种Syk抑制剂，IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果低5倍。Phase 3。 |
B cells were stimulated by irradiated CD40L+ L cells. Forward scatter vs. BrdU incorporation analysis (day 5) in the gated CD19+ CLL cells (D). The distribution of cells with high FSC (blasts, right quadrants) and proliferation (BrdU+, upper quadrants) are shown.
|
|
| S3026 |
PiceatannolPiceatannol，是一种天然二苯乙烯，是选择性Syk抑制剂，比作用于Lyn选择性高10倍左右。 |
Change of protein and mRNA with or without the pretreatment of Syk inhibitors. After pretreated with PRT062607 and Piceatannol for 30 min before A. fumigatus hyphae stimulation, activation of Syk was inhibited by 1 μM PRT062607 (p < 0.05), 2 μM PRT062607 (p < 0.01), 5 μM Piceatannol (p < 0.05), 10 μM Piceatannol (p < 0.01) a compared with untreated cells. mRNA expression of IL-1β, IL-6, IL-8 and CXCL1 induced by A. fumigatus hyphae were significantly suppressed b. mRNA expression of IL-1β, IL-6, IL-8, CXCL1 downregulated significantly by 1 μM PRT062607, 2 μM PRT062607, 5 μM Piceatannol, 10 μM Piceatannol. **means p < 0.01, *p < 0.05. |
|
| S4921 |
MNS (3,4-Methylenedioxy-β-nitrostyrene)MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)是一种酪氨酸激酶抑制剂，抑制Syk， Src和p97， IC50分别为2.5 μM， 29.3 μM和1.7 μM。 |
WT mouse primary macrophages were untreated as control (lane 1) or treated with 0.1μg/ml E. coli LPS (lane 5-8), 10μM E-64 (lane 2 and 6), 250μM PMSF (lane 3 and 7), or 20μM MNS (lane 4 and 8). The cells were continuously cultured for 16 hrs. Extracts from whole cells or nuclei were separately purified and subjected to WB analysis with antibody against pERK2, LITAF, or actin/tubulin as control.
|
|
| S7286 |
RO9021RO9021有效地抑制Syk激酶活性，IC50为5.6nM。它还能够抑制B细胞受体信号通路。 |
||
| S6519 |
R112R112是ATP竞争性Syk抑制剂，Ki值为96 nM。 |
||
| S3226 |
Dehydroabietic acidDehydroabietic acid (DAA, DHAA) 是一种天然的二萜树脂酸，衍生自针叶植物（如 Pinus 和 Picea）通过抑制 Src、Syk 和 TAK1 介导的通路来产生抗炎活性。 |
||
| S4944 |
Fostamatinib disodium hexahydrateFostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate 是活性代谢产物R406的前药，是一种 Syk 的抑制剂，在无细胞分析中的IC50值为41 nM。 |
||
| S0871 |
Gusacitinib (ASN-002)Gusacitinib (ASN-002) 是一种新型有效的脾酪氨酸激酶 (SYK) 和 Janus 激酶 (JAK) 双重抑制剂，在生化试验中 IC50 值为 5-46 nM。 |
||
| S8442 |
TAK-659TAK-659是一种有效的、选择性的SYK抑制剂。IC50为3.2 nM。对其他激酶具有选择性，对FLT3也能有效抑制，IC50为4.6 nM。 |
||
| S7738 |
PRT-060318 2HClPRT-060318 (PRT318) 是一种新型选择性Syk酪氨酸激酶抑制剂，IC50为4 nM。是一种肝素诱导性血小板减少症的治疗方法。 |
||
| S9715 |
Lanraplenib (GS-9876)Lanraplenib (GS-9876, GS-SYK) 是一种有效的、高选择性的 Spleen Tyrosine Kinase (SYK) 的口服活性抑制剂，其IC50值为9.5 nM。Lanraplenib 通过 glycoprotein VI (GPVI) receptor 抑制血小板中的SYK活性，而不会延长猴子或人类的出血时间(BT)。 |
||
| S8948 |
SRX3207SRX3207 是一种口服活性的 Syk-PI3K 的双重抑制剂，对 Syk、Zap70、BRD41、BRD42、PI3K alpha、PI3K delta、PI3K gamma 的IC50值分别为39.9 nM、31200 nM、3070 nM、3070 nM、244 nM、388 nM、9790 nM。SRX3207 会阻断肿瘤免疫抑制并增加抗肿瘤免疫力。 |
||
| S3566 |
Cerdulatinib (PRT062070)Cerdulatinib (PRT-062070, PRT2070) 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
||
| S7634 |
Cerdulatinib (PRT062070) hydrochlorideCerdulatinib (PRT-062070, PRT2070) hydrochloride 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
||
| S7523 |
Entospletinib (GS-9973)Entospletinib (GS-9973)是一种口服具有生物活性的，选择性Syk抑制剂，无细胞试验中IC50为7.7 nM。在细胞中，对Syk的选择性比对其他激酶（如Jak2, ckit, Flt3, Ret, KDR）高13-1000倍。 |
Dose titration effects of sotrastaurin (Sotr), GS-9973 (GS) on GSK-3 and AKT phosphorylation were evaluated in anti-IgM-stimulated CLL cells. One representative experiment out of 3 performed is shown.
|
|
| S7006 |
BAY-61-3606BAY-61-3606是一种有效的、选择性的Syk激酶抑制剂，Ki为7.5 nM。BAY-61-3606可诱导细胞周期阻滞和凋亡。 |
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