arthritis

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7 0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Tocilizumab (Anti-Human IL6R) is a neutralizing antibody against human interleukin-6 receptor (IL-6R) that blocks the binding of IL-6 to IL-6R, thereby inhibiting both classical and trans signaling. It can be used to study rheumatoid arthritis and has been suggested as a possible drug for the treatment of severe COVID-19.

Flurbiprofen (dl-Flurbiprofen) is an anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

Oxaceprol (N-Acetyl-L-hydroxyproline) is an established therapeutic agent for osteoarthritis.

TAK-715 is a p38 MAPK inhibitor for p38α.

Cinchophen (Cinconal), an analgesic drug, is utilized in treating gout.

UCB-9260 inhibits TNF signaling by stabilizing an asymmetric form of the trimer.

Etofenamate is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of joint and muscular pain.

Betahistine (Vasomotal) is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers. Betahistine dihydrochloride is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.

Betahistine EP Impurity C (NSC19005) is structurally related to Betahistine and is a dimer of Betahistine.

Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1 2 (IC50: 2 nM).

Clematichinenoside AR exerts anti-inflammatory and immunosuppressive properties, it has anti-arthritic effects on PI3K Akt signaling pathway and TNF-α± associated with collagen-induced arthritis.

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3 2 1 (IC50=1 20 112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

Ozoralizumab (ATN-103) is a humanized anti-TNFα antibody and a novel TNFα inhibitor.Ozoralizumab binds human serum albumin and can be used to study rheumatoid arthritis.

Adalimumab (anti-TNF-alpha) is the first fully human recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha.

Infliximab is a monoclonal antibody, a human-mouse chimeric monoclonal antibody that inhibits TNF-α and prevents TNF-α from interacting with TNFR1 and TNFR2. Infliximab can be used to treat Crohn's disease and rheumatoid arthritis.

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

DHODH-IN-13 is an inhibitor of DHODH with IC50 of 4.3 μM for rat liver. DHODH-IN-13 can be used in studies about rheumatoid arthritis.

DHODH-IN-14 is an analog of hydroxyfuran pyrimidine A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor IC50 0.49 μM mouse liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis.

DHODH-IN-15 is the hydroxyfuran analogue of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis.