Syk

Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

Entospletinib (GS-9973) is a Syk inhibitor (IC50=7.7 nM) with selective, oral activity. Entospletinib has potential value in the treatment of a variety of hematological malignancies and immune-related diseases.

Asebogenin is a compound fractionated from Salvia miltiorrhiza with antifungal activity, inhibition of GPVI-induced platelet reactions, and inhibition of NET formation induced by pro-inflammatory stimuli.

Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulatory activities.

Syk-IN-3 is a Syk inhibitor with potential anti-inflammatory and anticancer activity and can be used to study immune dysregulation.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

R406 (R-406 besylate) is an effective Syk inhibitor (IC50: 41 nM) and shows no effects on Lyn.

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

R406 free base (R406 (free base)) is a potent Syk inhibitor.

BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.

Cevidoplenib dimesylate is an inhibitor of spleen tyrosine kinase (Syk), possessing anti-inflammatory and immunomodulating properties.

PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.

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

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.

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM 6 nM 8 nM 0.5 nM and 32 nM for JAK1 JAK2 JAK3 TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

Linocinnamarin (3-[4-(beta-D-Glucopyranosyloxy)phenyl]acrylic acid methyl ester) is isolated from Fragaria ananassa Duch. (strawberry). The inhibition of antigen-stimulated degranulation by LN is mainly due to inactivation of Syk/phospholipase Cgamma (PLCgamma) pathways.

SRX3207 is an inhibitor of Syk and PI3K and relieves tumor immunosuppression.

MNS is a tyrosine kinases inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

Dehydroabietinol (Pomiferin A) inhibits growth of chloroquine-sensitive as well as chloroquine-resistant strains of Plasmodium falciparum cultivated in erythrocytes in vitro (IC 50 26-27 microM).