Syk
Spleen tyrosine kinase
Syk (Spleen tyrosine kinase) is a cytosolic non-receptor protein tyrosine kinase (PTK) that is expressed at high levels, both in hematopoietic cells (such as mast cells, B lymphocytes, T lymphocytes, neutrophils, dendritic cells, and macrophages) and in non-hematopoietic cells.
Syk mediates key signal transduction pathways following the activation of immune cell receptors. Syk associates with different receptors on the surface of various cells such as B cells, mast cells, monocytes, macrophages, and neutrophils, and even osteoclasts and breast cancer cells. Following the engagement of these receptors with their ligands, SYK is activated and orchestrates diverse cellular responses, including cytokine production (in T cells and monocytes) and phagocytosis (in macrophages).
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Syk Produits associés (99)
Produits associés (99)
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R406
0 ImagesCat. No.: HY-12067CAS No.: 841290-81-1R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
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Fostamatinib
0 ImagesSynonyms: R788
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Piceatannol
0 ImagesSynonyms: Astringenin; trans-PiceatannolPiceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI). Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties. Piceatannol induces apoptosis in DLBCL cell lines. Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells.
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PRT062607
0 ImagesSynonyms: P505-15; PRT-2607; BIIB-057PRT062607 (P505-15; PRT-2607) is an orally active ATP-competitive Syk inhibitor with an IC50 value of 1 nM, and exhibits at least 80-fold selectivity over other kinases. PRT062607 blocks B cell antigen receptor-mediated activation, Fcε receptor 1-mediated basophil degranulation and microglial phagocytosis, and induces caspase-dependent apoptosis and microglial death. PRT062607 inhibits tumor growth and peripheral nerve injury-induced mechanical allodynia, and prevents neuronal loss. PRT062607 can be used in research related to rheumatoid arthritis, chronic lymphocytic leukemia, non-Hodgkin's lymphoma, neurodegenerative diseases and neuropathic pain.
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As48
0 ImagesCat. No.: HY-182702CAS No.: 1214405-38-5As48 is a selective TREM2 agonist with a KD value of 12.48 μM in TRIC binding assay. As48 binds near the TREM2 cleavage region, forms hydrogen bonds with Gly68, reduces conformational flexibility in regions 58-102, restricts protease accessibility to the cleavage site. As48 activates SYK phosphorylation, enhances microglial phagocytosis, and induces downstream calcium signaling in TREM2-expressing cells. As48 inhibits TREM2 ectodomain shedding without affecting ADAM10/17 protease activities. As48 can be used for the research of Alzheimer's disease.
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Vexicitinib
0 ImagesCat. No.: HY-184063CAS No.: 2230362-69-1Synonyms: Vexicitinibum
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Syk/HDAC6-IN-1
0 ImagesCat. No.: HY-184415Syk/HDAC6-IN-1 is a dual SYK/HDAC6 selective inhibitor with IC50 values of 0.19 nM (SYK) and 0.66 nM (HDAC6). Syk/HDAC6-IN-1 downregulates p-SYK to block downstream AKT/FOXO1 signaling, elevates acetylated histone H3 and α-tubulin via HDAC suppression, represses SREBF1 -mediated lipid biosynthetic pathways, triggers G0/G1 cell cycle arrest and robust mitochondrial-dependent caspase-3-mediated apoptosis in leukemia cells. Syk/HDAC6-IN-1 can be used for the research of FLT3-mutant acute myeloid leukemia.
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BAY 61-3606 dihydrochloride
0 ImagesBAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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R406 free base
0 ImagesR406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
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PRT062607 Hydrochloride
0 ImagesSynonyms: P505-15 Hydrochloride
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Gusacitinib
0 ImagesSynonyms: ASN-002Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.
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Mivavotinib monohydrochloride
0 ImagesSynonyms: TAK-659 monohydrochloride; CB-659 monohydrochlorideTAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
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Lanraplenib
0 ImagesSynonyms: GS-9876Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
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Alisol B 23-acetate
0 ImagesSynonyms: 23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetateAlisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma.
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PRT-060318
0 ImagesSynonyms: PRT318PRT-060318 (PRT318) s a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 prevents Heparin (HY-17567)-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.
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Flavanomarein
0 ImagesFlavanomarein is a substance with cytoprotective, anti-inflammatory and antioxidant activities, with a Ka of 3.064e-5 M against human Syk. Flavanomarein enhances the phosphorylation level of AKT, regulates the expression of PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2 and ICAD, and inhibits the nuclear translocation of NF-κB p65. Flavanomarein regulates EMT marker proteins, promotes the proliferation of HK-2 cells, and protects neuronal cells from 6-OHDA-induced neurotoxic damage. Flavanomarein can be used in studies related to Parkinson's disease and diabetic nephropathy.
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Syk Inhibitor II
0 ImagesSyk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
