syk-in-1

Syk-IN-11 is a selective Syk inhibitor.

SYK/JAK-IN-1 is a dual SYK/JAK inhibitor with IC50 values of less than 5 nM for both SYK and JAK2.

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb-/-) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb-/- macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb-/- mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

BTK-IN-34 (compound 9h; 1-50 μM; 24 小时) reduces levels of pBTK, pERK 1 2 (Thr202 Tyr204), and p-p38 (Thr180 Tyr182) in RAMOS cells [1]. This compound shows selective cytotoxicity towards BTK-high RAMOS cells with an IC50 of 2.75 μM. Western Blot analysis was conducted on RAMOS cells with concentrations of 1 μM, 10 μM, and 50 μM over a 24-hour incubation, resulting in decreased pBTK (Tyr223) levels.

Syk-IN-8 (compound 19q) is a Syk inhibitor with demonstrated antiproliferative effects on various hematological tumor cells, specifically inhibiting PLCγ2 phosphorylation and applicable in blood cancer research [1].

Syk-IN-4 is a potent, selective, and orally bioavailable inhibitor of SYK, with an IC50 of 0.31 nM, targeting SYK, a potential therapeutic target for autoimmunity and hematological cancers[1].

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

Syk-IN-7 (compound 17) acts as an inhibitor of spleen tyrosine kinase (SYK) [1].

Glaucocalyxin A diacetate is a natural product for research related to life sciences. The catalog number is TN6258 and the CAS number is 79498-37-6.