Syk Inhibitor

PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC₅₀ of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin (HY-17567)-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.

Syk-IN-1 (compound 4) is a potent Syk inhibitor, with an IC₅₀ of 35 nM.

Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect.

ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC₅₀ of 10 μM and can be used for study in allergic diseases.

E8431 is a DCSTAMP antagonist with an IC₅₀ value of 775.8 nM for osteoclastogenesis. E8431 selectively binds to the endoplasmic reticulum domain of DCSTAMP, disrupts its interaction with RAP1B, and inhibits downstream cytoskeleton rearrangement mediated by the RAP1-RAC1 signaling pathway, thereby impeding osteoclast precursor fusion, suppressing bone resorption, and stimulating PDGFBB secretion to promote osteogenesis and angiogenesis. E8431 can be used in the research of osteoporosis.

BI1002494 is an orally active, potent, and selective spleen tyrosine kinase (SYK) inhibitor. BI 1002494 exhibits an IC₅₀ of 115 nM in inhibiting high-affinity IgE receptor-mediated mast cell and basophil degranulation. BI1002494 can be utilized in immunology reesearch.

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

Piceatannol (Standard) is the analytical standard of Piceatannol. This product is intended for research and analytical applications. 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.

TAK-659 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 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC₅₀=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

Gusacitinib (ASN-002) hydrochloride 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 hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.

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.

Syk/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.

Syk Inhibitor II hydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II hydrochloride inhibits 5-HT release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II hydrochloride shows less potent against other kinases and has anti-allergic effect.

GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC₅₀=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC₅₀ of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC₅₀s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.

SYK-IN-15 is an orally active spleen tyrosine kinase (SYK) inhibitor with an IC₅₀ of 10.9 nM. SYK-IN-15 induces cell cycle S-phase arrest and cell apoptosis. SYK-IN-15 inhibits cancer cell colony formation and exerts antiproliferative effects on cancer cells. SYK-IN-15 can be used for the research of solid tumors (ovarian cancer, breast cancer, liver cancer).

Syk-IN-8 (compound 19q) is a Syk inhibitor, with antiproliferative activity against multiple hematological tumour cells. Syk-IN-8 inhibits PLCγ2 phosphorylation, can be used for research in blood cancers.

TOP1362 is a narrow spectrum kinase inhibitor. TOP1362 is a potent inhibitor of P38-α and Syk kinases with K_d values of 26 and 18 nM, respectively and an IC₅₀ of 14 nM in the Src kinase activity assay. TOP1362 potently inhibits P38-α, Src and Syk. TOP1362 can be used in the research of dry eye syndrome.

DBMB is an inhibitor of spleen tyrosine kinase (Syk), capable of significantly inhibiting the activity of Syk kinase. DBMB exhibits anti-inflammatory activity by suppressing the signaling of NF-κB, which in turn reduces the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB can be utilized in research on inflammatory diseases.