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.

L-161982 is a selective EP4 receptor antagonist that inhibits PGE2-induced ERK phosphorylation and cell proliferation in HCA-7 cells and alleviates collagen-induced arthritis in mice.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Betahistine dihydrochloride (Betahistine 2HCl) is a histamine analog and H1 receptor agonist that serves as a vasodilator.

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.

Sulfinpyrazone (NSC-75925) is a uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.

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

Aceclofenac (Preservex) is a non-steroidal anti-inflammatory drug (NSAID) with marked anti-inflammatory and analgesic properties.

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.

Tiaprofenic acid (Acido tiaprofenico) is a non-steroidal anti-inflammatory drug used to treat pain, especially arthritic pain.

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

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

CD80-IN-3 is a potent CD80 inhibitor and inhibits CD80/CD28 interaction (Kd: 125 nM; EC50: 630 nM).

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

RWJ 50271 is a selective lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction inhibitor( IC50 of 5.0 μM in HL60 cells).

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

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

BVT 2733 is a new, non-steroidal, isoform-specific inhibitor of 11β-HSD1.

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

Pectolinarin is a Cirsium isolate with anti-inflammatory activity.

S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.