Syk

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

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

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

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

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.

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).

TAK-659 hydrochloride (TAK-659) is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.

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

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

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.

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.

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

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

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.

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.

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.

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

R112 is an ATP-competitive inhibitor of Syk kinase. Ki=6 nM,IC50=226 nM.

Sovleplenib (HMPL523) is an orally available, selective and potent inhibitor of the splenic tyrosine kinase SYK with an IC50 of 25 nM.Sovleplenib has antitumor activity and may be used in studies of immune thrombocytopenia (ITP).

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

BAY 61-3606 dihydrochloride (BAY 61-3606) is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).

Anthraquinone-2-carboxylic acid acts as a potent anti-inflammatory and antinociceptive component in vivo, thus contributing to the immune regulatory role of fruits and herbs.

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

Cevidoplenib dimesylate hydrochloride is a spleen tyrosine kinase (Syk) inhibitor showing potential immunomodulating and anti-inflammatory properties.

TC-S 7003 (Lck Inhibitor) is an orally active, selective and potent lymphocyte kinase (Lck) inhibitor with anti-inflammatory activity, inhibition of Lck, Lyn, Src, and Syk kinases, and inhibition of T-cell proliferation, and may be useful in the study of arthritis.

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].

TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM), showing >70% inhibition of Syk and four other kinases [FLT3 (IC50: 10 nM), JAK2 (IC50: 4.8 nM), KDR (IC50: 600 nM), RET (IC50: 29 nM)] in a panel of 192 kinases.

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

ER-27319, an acridone derivative, serves as a potent and selective inhibitor of spleen tyrosine kinase (SYK), effectively impeding both the tyrosine phosphorylation and enzymatic activity of SYK. With an inhibitory concentration (IC50) of 10 µM, this compound suppresses the release of allergic mediators from human and rat mast cells triggered by antigens, making it useful for allergy research [1] [2].

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

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

OXSI-2 (Syk Inhibitor) is an inhibitor of Syk with an EC50 of 313 nM and an IC50 of 14 nM. OXSI-2 completely inhibits Adaptor protein LAT Y191 phosphorylation and Syk mediated events in platelets.