synovial

Rapanone (2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone) is a natural benzoquinone that is a potent and selective inhibitor of human synovial PLA2.

NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.

Hyaluronic acid (hyaluronan) is a glucosaminoglycan consisting of D-glucuronic acid and N-acetyl-D-glucosamine disaccharide units that is a component of connective tissue, skin, vitreous humour, umbilical cord, synovial fluid and the capsule of certain microorganisms contributing to adhesion, elasticity, and viscosity of extracellular substances.

DNJNAc, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of β-hexosaminidase (HEX). HEX enzymes catalyze the hydrolysis of terminal non-reducing N-acetyl-β-D-glucosamine (GlcNAc) and N-acetyl-β-D-galactosamine (GalNAc) residues from glycoconjugates such as glycoproteins, gangliosides, and glycosaminoglycans. HEX secreted by chondrocytes into the extracellular space contributes to cartilage matrix degradation, and HEX activity is elevated in the synovial fluid of osteoarthritis patients.

SXT1596 is a novel SS18-SSX/TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.

Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), effectively blocking HIF-1 signaling and promoting the degradation of HIF-1α. It inhibits synovial invasion and migration, as well as angiogenesis. In mouse inflammation models, Anti-inflammatory agent 79 effectively reduces foot swelling and arthritis and lowers levels of inflammatory factors and angiogenesis in vivo.

SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.

Fce 21258 is used to stimulate the adenylate cyclase of synovial fluid macrophages.

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.

Resolvin D5 is an oxidised lipid mediator derived from docosahexaenoic acid (DHA) with anti-inflammatory properties. It inhibits the production of interleukin-6 (IL-6) and chemokine CCL5 in LPS-stimulated THP-1 cells via the ERK-NF-κB signalling pathway.

9(E)-Octadecenamide (Elaidamide) is a fatty acid amide and endogenous metabolite that inhibits rat microsomal epoxide hydrolase (mEH) with a Ki of 70 nM.

S-methyl-KE-298 is the second main metabolite in plasma,is a methyl conjugate of deacetyl-KE-298.KE-298 inhibits matrix metalloproteinase (MMP-1) production from  rheumatoid arthritis (RA) synovial cells.

Oxaprozin potassium is an orally active and potent inhibitor of COX, with IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. It induces cell apoptosis and inhibits NF-κB activation. The inhibition of the Akt/IKK/NF-κB pathway by oxaprozin potassium contributes to its anti-inflammatory properties [1] [2].

AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg/kg (ED(50)=0.053 mg/kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this stu......

AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury.

FPTI is an inhibitor against SYT-SSX1 fusion protein in synovial sarcoma which down-regulates SYT-SSX1 and modulates its downstream target genes.

BE-16627B is a novel metalloproteinase (MP) inhibitor isolated from Streptomyces sp. BE16627B selectively inhibited MPs such as human stromelysin and 92 kD gelatinase. After the cells were cultured with BE16627B for 5 days, BE16627B inhibited MP activity in the primary culture supernatants from synovial cells in a dose-dependent fashion without showing apparent cytotoxicity or affecting the production and secretion of MPs. Its IC50 for active collagenolysis before activation by trypsin was 25 microM.

FHD-609 is an effective BRD9 inhibitor and PROTAC degrader, targeting the non-classical BAF (ncBAF) subunit BRD9, thereby depleting the SS18-SSX fusion protein, and can be used for the study of synovial sarcoma (SS).

Tabituximab barzuxetan (OTSA101-DTPA-90Y) is a radioimmunoconjugate composed of a humanized monoclonal antibody targeting FZD-10 (OTSA-101) , and labeled with Yttrium 90. Tabituximab barzuxetan shows antineoplastic activity. Tabituximab barzuxetan can be used for synovial sarcoma research [1] .

TNO211 is a bioactive peptide that functions as a highly soluble fluorogenic substrate for select Matrix Metalloproteinases (MMPs)—specifically MMP-2, 8, 12, 13, and 14. Incorporating a cleavable Gly-Leu bond and an EDANS/DABCYL fluorophore/quencher pair, TNO211 enables sensitive detection of MMP activity through fluorescence assays, with an absorption/emission profile at 340/490 nm. It is particularly effective in analyzing MMPs in culture media from endothelial cells as well as untreated synovial fluid from patients, highlighting its utility in investigations of MMP-associated cellular behaviors, including proliferation, migration (adhesion/dispersion), differentiation, angiogenesis, apoptosis, and host defense.

HAP-1, a synovial-targeted transduction peptide, selectively mediates the internalization of protein complexes into synovial cells of human and rabbit origin. When fused with the antimicrobial peptide (KLAK)2, HAP-1 forms the proapoptotic peptide DP2 [1].

1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.

PDE4-IN-18 (compound 1l) is a PDE4 inhibitor with an IC50 value of 1.55 μM and exhibits anti-inflammatory activity. It mitigates inflammation by reducing excessive infiltration of immune cells and enthesial formation, as well as decreasing the mRNA expression of pro-inflammatory cytokines (such as TNF-α and IL-6) in the synovial tissues. PDE4-IN-18 is suitable for research into rheumatoid arthritis and psoriasis.

Pronqodine A is a quinone isolated from Streptomyces, known for its enzyme inhibitory and anti-inflammatory properties. It targets NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1; IC50 = 131.5 nM). In SW 982 human synovial sarcoma cells, it suppresses bradykinin-induced production of prostaglandin E2 (PGE2), 6-keto PGF1α, and PGD2, with IC50 values of 9, 19, and 7 nM, respectively, and it also promotes the generation of reactive oxygen species (ROS) in these cells.