Syk Inhibitor

R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

Fostamatinib (R788) is the oral proagent of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a K_i of 30 nM and an IC₅₀ of 41 nM. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

Piceatannol 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.

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC₅₀ of 7.7 nM.

PRT062607 (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.

Vexicitinib (Vexicitinibum) is a SYK and JAK2 inhibitor with IC₅₀ values both less than 10 nM. Vexicitinib exhibits anti-inflammatory and immunosuppressive effects. Vexicitinib can be used in tumor-related research.

Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC₅₀ of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC₅₀s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.

BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K_i 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.

PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC₅₀: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models.

R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

Gusacitinib (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.

TAK-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).

Lanraplenib (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.

Alisol 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.

PRT-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.

Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC₅₀ of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP).

Flavanomarein is a substance with cytoprotective, anti-inflammatory and antioxidant activities, with a K_a 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.

Syk 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.

MNS (NSC 170724), the beta-nitrostyrene derivative, is an orally active tyrosine kinase inhibitor, a broad-spectrum antiplatelet agent, and a PANoptosis inhibitor. MNS inhibits Src, Syk, and FAK with IC₅₀ of 27.3, 2.8, and 97.6 μM, respectively. MNS inhibits NLRP3 inflammasome and β1 integrin. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC₅₀ values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS is cytotoxic to a variety of cells.

BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.