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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4209 |
TAK-659 hydrochloride
TAK-659 |
VEGFR; FLT; Tyrosine Kinases; JAK; Syk | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
TAK-659 hydrochloride (TAK-659) 是可逆的、高效的、选择性的、口服有效的 SYK/FLT3 双抑制剂,对 SYK 和 FLT3 作用的IC50值分别为 3.2 nM、4.6 nM。它能诱导肿瘤细胞死亡,却不作用于非肿瘤细胞,对慢性淋巴细胞白血病具有潜在的研究价值。 | |||
T39437 |
Cevidoplenib dimesylate
|
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Cevidoplenib dimesylate 是一种脾酪氨酸激酶 (Syk) 抑制剂,具有抗炎和免疫调节特性。 | |||
T16776 |
RO9021
|
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
RO9021 是口服具有活力的,ATP 竞争性的 SYK 抑制剂,其 IC50=5.6 nM。 | |||
T14331 |
Gusacitinib
ASN-002 |
JAK; Syk | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Gusacitinib (ASN-002) 是一种有效的 SYK 激酶和JAK 激酶的双抑制剂,IC50值为 5 到 46 nM 之间,具有抗癌活性。 | |||
T6594 |
MNS
|
Syk; Src; p97 | Angiogenesis; Tyrosine Kinase/Adaptors; Ubiquitination |
MNS 是一种酪氨酸激酶抑制剂和广谱抗血小板药物,是一种 β-硝基苯乙烯衍生物。它完全抑制 U46619 (IC50:2.1 μM)、ADP (IC50:4.1 μM)、花生四烯酸 (IC50:5.8 μM)、胶原 (IC50:7.0 μM)和凝血酶 (IC50:12.7 μM)诱导的血小板聚集,并抑制 Src (IC50:27.3 μM)、Syk (IC50:2.8 μM) 和 FAK (IC50:97.6 μM)。 | |||
T11824LL |
Lanraplenib
GS-9876 |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Lanraplenib (GS-9876) 是高效的、选择性的、口服具有活力的 SYK 抑制剂 (IC50=9.5 nM) ,能够用于炎症性疾病的研究。它通过糖蛋白 VI (GPVI) 受体抑制血小板中的 SYK 活性,而不会延长猴子或人类的出血时间 (BT)。 | |||
T6101 |
Entospletinib
GS-9973 |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Entospletinib (GS-9973) 是选择性的Syk 抑制剂,其IC50=7.7 nM。 | |||
T6115 |
Fostamatinib
R788,福他替尼 |
FLT; Syk; Monoamine Transporter; Adenosine Receptor | Angiogenesis; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors |
Fostamatinib (R788) 是一种口服具有活力的 R406 前药。其中R406 是具有口服活性的,有效的,ATP 竞争性的Syk/FLT3抑制剂(Ki:30 nM,IC50:41 nM),也能够抑制 Lyn (IC50:63 nM) 和 Lck (IC50:37 nM)。 | |||
T6174 |
R406
R-406 besylate |
Apoptosis; FLT; Syk | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
R406 (R-406 besylate) 是一种具有口服活性的 ATP 竞争性 Syk/FLT3抑制剂,Ki 为 30 nM。它有效抑制 Syk 激酶活性,IC50为 41 nM。它还抑制 Lyn 和 Lck,IC50值分别为 63 nM 和 37 nM。它可减轻免疫复合物介导的炎症。 | |||
T2467 |
R406 free base
R406 (free base) |
Apoptosis; FLT; Syk | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
R406 free base (R406(free base)) 是一种具有口服活性的,ATP 竞争性的Syk/FLT3抑制剂,Ki 为 30 nM。它有效抑制 Syk 激酶活性,IC50为 41 nM,可减轻免疫复合物介导的炎症。它还抑制 Lyn 和 Lck,IC50分别为 63 nM 和 37 nM。 | |||
T4348 |
Syk Inhibitor II
|
5-HT Receptor; Syk | Angiogenesis; GPCR/G Protein; Neuroscience; Tyrosine Kinase/Adaptors |
Syk Inhibitor II 是一种可渗透细胞、具有 ATP 竞争性的嘧啶-甲酰胺化合物,可选择性且可逆地抑制 Syk,IC50为 41 nM。 | |||
T2487 |
Cerdulatinib
PRT2070,赛度替尼,PRT062070 |
Tyrosine Kinases; JAK; Syk | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Cerdulatinib (PRT2070) 是一种选择性 Tyk2抑制剂,IC50为 0.5 nM。它是 JAK 和 SYK 的双抑制剂,抑制JAK1、2、3 和SYK 的IC50分别为12、6、8 和 32。 | |||
T3185 |
R112
(E)-Elafibranor |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
R112 ((E)-Elafibranor) 是ATP 竞争性的 Syk 激酶抑制剂,它能够抑制Syk 激酶活性,Ki=6 nM,IC50=226 nM。 | |||
T6957 |
PRT-060318
P142-76,PRT318,PRT-060318 2HCl |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
PRT-060318 (P142-76) 是一种新颖的、选择性的酪氨酸激酶 (Syk) 抑制剂,其IC50=4 nM。 | |||
T2605 |
Fostamatinib Disodium
Tamatinib Fosdium,福他替尼二钠盐,R788(Disodium),R788 Disodium,R788 (Fostamatinib) Disodium |
FLT; Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Fostamatinib Disodium (R788 Disodium) 是一种口服具有活力的 R406 前药。其中R406 是具有口服活性的,有效的,ATP 竞争性的Syk/FLT3抑制剂(Ki:30 nM,IC50:41 nM),也能够抑制 Lyn (IC50:63 nM) 和 Lck (IC50:37 nM)。 | |||
T6776 |
BAY 61-3606 dihydrochloride
BAY 61-3606,BAY-61-3606 dihydrochloride |
Apoptosis; Syk | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
BAY 61-3606 dihydrochloride (BAY 61-3606) 是一种口服有效的,ATP 竞争性的,可逆的选择性Syk 抑制剂。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化,也降低 K-rn 细胞裂解物中 Syk 磷酸化。它作用于乳腺癌细胞,通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。 | |||
T2696 |
PRT062607 hydrochloride
PRT062607 (P505-15, BIIB057) HCl,P505-15 Hydrochloride |
MLK; Syk; Src | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
PRT062607 hydrochloride (P505-15 Hydrochloride) 是纯化的 Syk 抑制剂,IC50=1-2 nM。 | |||
T4263 |
BAY 61-3606
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺,Syk inhibitor IV |
Apoptosis; Syk | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
BAY 61-3606 (Syk inhibitor IV) 是一种具有口服活性的,ATP 竞争性的可逆选择性Syk 抑制剂。它作用于乳腺癌细胞,通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化,也降低 K-rn 细胞裂解物中 Syk 磷酸化。 | |||
T6104 |
Cerdulatinib hydrochloride
Cerdulatinib,PRT2070,PRT062070 hydrochloride,PRT062070,PRT2070 hydrochloride |
MLK; c-Fms; Tyrosine Kinases; Hippo pathway; JAK; Syk | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Stem Cells; Tyrosine Kinase/Adaptors |
Cerdulatinib hydrochloride (PRT2070 hydrochloride) 是一种选择性可逆,具有口服活性、 ATP 竞争性的 SYK 和 JAK 的双重抑制剂,抑制 JAK1、2、3、SYK 和 Tyk2的 IC50值分别为12、6、8、32 和 0.5 nM。它可用于研究自身免疫性疾病和B 细胞恶性肿瘤。 | |||
T28281 |
OXSI-2
OXSI 2,Syk Inhibitor |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
OXSI-2 (Syk Inhibitor) 是 Syk 的抑制剂,EC50 为 313 nM,IC50 为 14 nM。 OXSI-2 完全抑制适配器蛋白 LAT Y191 磷酸化和 Syk 介导的血小板聚集。 | |||
T9789 |
Cevidoplenib dimesylate hydrochloride
|
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Cevidoplenib dimesylate hydrochloride 是一种脾酪氨酸激酶 (Syk) 抑制剂,具有潜在的免疫调节和抗炎特性。 | |||
T9659 |
LCB 03-0110
3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol |
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
LCB 03-0110 (3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol) 是一种盘状结构域受体家族酪氨酸激酶的强效抑制剂,可强烈抑制多种酪氨酸激酶,包括 c-Src 家族、脾酪氨酸激酶、布鲁顿酪氨酸激酶和血管内皮生长因子受体 2,它们对免疫很重要细胞信号传导和炎症反应。 | |||
T24584 |
P505-15 Acetate
PRT 062607 Acetate,P505 15 Acetate,PRT-062607 Acetate,PRT062607 Acetate,P50515 Acetate |
Tyrosinase | Proteases/Proteasome |
P505-15 Acetate 是脾脏酪氨酸激酶的选择性抑制剂,通过抑制白细胞免疫功能和炎症起作用,导致关节炎评分降低和组织学损伤减轻。 | |||
T4391 |
Syk Inhibitor II dihydrochloride
Syk Inhibitor II (hydrochloride) |
Others; Tyrosine Kinases; Syk; PKC; BTK | Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling; Others; Tyrosine Kinase/Adaptors |
Syk Inhibitor II (hydrochloride) 是一种非受体酪氨酸激酶,磷酸化后,它与 FcRγ 链的基于免疫受体酪氨酸的激活基序结合,并介导与血小板功能和炎症相关的下游信号传导。 Syk inhibitor II 是一种可渗透细胞的嘧啶-甲酰胺化合物,以 ATP 竞争性方式选择性和可逆地阻断 Syk (IC50 = 41 nM)。它对 PKCε、PKCβII、ZAP-70、Btk 和 Itk 的效力要低得多(IC50s 分别为5.1、11、11.2、15.5 和 22.6 μM)。 | |||
T9543 |
Syk Inhibitor II hydrochloride
|
Others | Others |
Syk Inhibitor II hydrochloride 信号传导的影响在狼疮中可能很突出。 | |||
T70931 |
SYK-IN-II
|
||
SYK-IN-II is an inhibitor of the spleen tyrosine kinase (STK). | |||
T21062 |
TAK-659
TAK 659,TAK659 |
||
TAK-659 is a spleen tyrosine kinase (SYK) inhibitor. | |||
T37602 | GSK 143 | ||
Spleen tyrosine kinase (Syk) inhibitor (pIC50 = 7.5). Also inhibits phosphorylated Erk (pIC50 = 7.1). Decreases cell number and viability in chronic lymphocytic leukemia (CCL) cell lines. Liddle et al (2011) Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg.Med.Chem.Lett. 21 6188 PMID:21903390 |Varghese et al (2018) Highly selective SYK inhibitor, GSK143, abrogates survival signals in chronic lymphocytic leukaemia. Br.J.Haematol 182 9... | |||
T70994 | TAK-659 HCl | ||
TAK-659 is an inhibitor of spleen tyrosine kinase (syk), with potential anti-inflammatory, immunomodulating, and antineoplastic activities. Spleen tyrosine kinase inhibitor TAK-659 may inhibit the activity of syk, which abrogates downstream B-cell receptor (BCR) signaling and leads to an inhibition of B-cell activation, chemotaxis, adhesion and proliferation. Note: TAK-659 free base is less stable. This product is supplied as dihydrochloride form. | |||
T78943 |
Syk-IN-7
|
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Syk-IN-7(化合物17)是一类特定的酪氨酸激酶(SYK)抑制剂。 | |||
T70930 |
GSK SYK inhibitor
|
||
The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double-blind, multicentre, Phase Ib study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical efficacy of the selective SYK inhibitor GSK2646264 in active CLE lesions | |||
T39874 |
GSK143 dihydrochloride
|
||
GSK143 dihydrochloride is a highly selective, orally active inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC 50 value of 7.5. It effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. The compound demonstrates anti-inflammatory properties and hinders the recruitment of immune cells in the intestinal muscularis of mice. | |||
T61527 |
GSK2646264
|
||
GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. In addition to targeting SYK, GSK2646264 also inhibits several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B, and Aurora A, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3, respectively. Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1]. | |||
T38626 |
GSK143
|
||
GSK143 is a potent orally active and highly selective inhibitor of spleen tyrosine kinase (SYK) with a pIC 50 of 7.5. Furthermore, GSK143 effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. In addition, GSK143 exhibits promising anti-inflammatory properties by reducing inflammation and impeding the recruitment of immune cells in the intestinal muscularis of mice. | |||
T78641 | ER-27319 | Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
ER-27319为吖啶酮衍生物,高效选择性抑制SYK,阻断其酪氨酸磷酸化和活性。本化合物阻止抗原刺激下人及大鼠肥大细胞释放过敏介质,IC50约为10 μM,适用于过敏性疾病研究。 | |||
T70377 |
BAY 61-3606 HCl
|
||
BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used i... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0610 |
Piceatannol
白皮杉醇,trans-Piceatannol,Astringenin |
Apoptosis; Serine/threonin kinase; PKA; Syk; PKC; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism; Tyrosine Kinase/Adaptors |
Piceatannol (Astringenin) 是一种Syk 抑制剂,可降低由 TNF 诱导的 iNOS 表达,可研究急性肺损伤。它是存在于各种水果和蔬菜中天然存在的多酚二苯乙烯,可诱导细胞自噬和凋亡,具有抗癌和抗炎特性。 |