syk

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

Syk inhibitor II, a cell-permeable, ATP-competitive, pyrimidine-carboxamide compound, selectively and reversibly inhibits Syk (IC50 = 41 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.

RO9021 is an orally bioavailable, novel ATP-competitive SYK inhibitor [average IC50: 5.6 nM].

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.

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.

Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.

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.

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].

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

PRT062607 hydrochloride (P505-15 Hydrochloride) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.

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

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

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).

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

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

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

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.

Syk-IN-11 is a selective Syk inhibitor.

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].

SYK-IN-II is an inhibitor of the spleen tyrosine kinase (STK).

Syk Inhibitor II dihydrochloride dihydrate is a highly selective, potent, ATP-competitive Syk inhibitor (IC50: 41 nM) that exhibits anti-allergic effects.

Syk Kinase Peptide Substrate is a peptide specifically designed to act as a substrate for Syk kinase.

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