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36

抑制剂 & 化合物

1

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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...

化合物

TAK-659 hydrochloride
Cat.No: T4209
Synonym: TAK-659
Target: VEGFR, FLT, Tyrosine Kinases, JAK, Syk
Cevidoplenib dimesylate
Cat.No: T39437
Synonym:
Target: Syk
RO9021
Cat.No: T16776
Synonym:
Target: Syk
Gusacitinib
Cat.No: T14331
Synonym: ASN-002
Target: JAK, Syk
MNS
Cat.No: T6594
Synonym:
Target: Syk, Src, p97
Lanraplenib
Cat.No: T11824LL
Synonym: GS-9876
Target: Syk
Entospletinib
Cat.No: T6101
Synonym: GS-9973
Target: Syk
Fostamatinib
Cat.No: T6115
Synonym: R788,福他替尼
Target: FLT, Syk, Monoamine Transporter, Adenosine Receptor
R406
Cat.No: T6174
Synonym: R-406 besylate
Target: Apoptosis, FLT, Syk
R406 free base
Cat.No: T2467
Synonym: R406 (free base)
Target: Apoptosis, FLT, Syk
Syk Inhibitor II
Cat.No: T4348
Synonym:
Target: 5-HT Receptor, Syk
Cerdulatinib
Cat.No: T2487
Synonym: PRT2070,赛度替尼,PRT062070
Target: Tyrosine Kinases, JAK, Syk
R112
Cat.No: T3185
Synonym: (E)-Elafibranor
Target: Syk
PRT-060318
Cat.No: T6957
Synonym: P142-76,PRT318,PRT-060318 2HCl
Target: Syk
Fostamatinib Disodium
Cat.No: T2605
Synonym: Tamatinib Fosdium,福他替尼二钠盐,R788(Disodium),R788 Disodium,R788 (Fostamatinib) Disodium
Target: FLT, Syk
BAY 61-3606 dihydrochloride
Cat.No: T6776
Synonym: BAY 61-3606,BAY-61-3606 dihydrochloride
Target: Apoptosis, Syk
PRT062607 hydrochloride
Cat.No: T2696
Synonym: PRT062607 (P505-15, BIIB057) HCl,P505-15 Hydrochloride
Target: MLK, Syk, Src
BAY 61-3606
Cat.No: T4263
Synonym: 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
Target: Apoptosis, Syk
Cerdulatinib hydrochloride
Cat.No: T6104
Synonym: Cerdulatinib,PRT2070,PRT062070 hydrochloride,PRT062070,PRT2070 hydrochloride
Target: MLK, c-Fms, Tyrosine Kinases, Hippo pathway, JAK, Syk
OXSI-2
Cat.No: T28281
Synonym: OXSI 2,Syk Inhibitor
Target: Syk
Cevidoplenib dimesylate hydrochloride
Cat.No: T9789
Synonym:
Target: Syk
LCB 03-0110
Cat.No: T9659
Synonym: 3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol
Target: Discoidin Domain Receptor (DDR)
P505-15 Acetate
Cat.No: T24584
Synonym: PRT 062607 Acetate,P505 15 Acetate,PRT-062607 Acetate,PRT062607 Acetate,P50515 Acetate
Target: Tyrosinase
Syk Inhibitor II dihydrochloride
Cat.No: T4391
Synonym: Syk Inhibitor II (hydrochloride)
Target: Others, Tyrosine Kinases, Syk, PKC, BTK
Syk Inhibitor II hydrochloride
Cat.No: T9543
Synonym:
Target: Others
SYK-IN-II
Cat.No: T70931
Synonym:
Target:
TAK-659
Cat.No: T21062
Synonym: TAK 659,TAK659
Target:
GSK 143
Cat.No: T37602
Synonym:
Target:
TAK-659 HCl
Cat.No: T70994
Synonym:
Target:
Syk-IN-7
Cat.No: T78943
Synonym:
Target: Syk
GSK SYK inhibitor
Cat.No: T70930
Synonym:
Target:
GSK143 dihydrochloride
Cat.No: T39874
Synonym:
Target:
GSK2646264
Cat.No: T61527
Synonym:
Target:
GSK143
Cat.No: T38626
Synonym:
Target:
ER-27319
Cat.No: T78641
Synonym:
Target: Syk
BAY 61-3606 HCl
Cat.No: T70377
Synonym:
Target:
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。

天然产物

Piceatannol
Cat.No: T0610
Synonym: 白皮杉醇,trans-Piceatannol,Astringenin
Target: Apoptosis, Serine/threonin kinase, PKA, Syk, PKC, Autophagy
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