autoimmune

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.

Upadacitinib (ABT-494) is a highly potent, selective, and orally active JAK1 inhibitor with an IC₅₀ of 43 nM; its selectivity for JAK1 is approximately 74 times that for JAK2. Upadacitinib is being investigated for the treatment of autoimmune diseases such as rheumatoid arthritis and ankylosing spondylitis.

SN-011 (GUN35901) is a STING inhibitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease. It is a demethyl analogue of DUN99845.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate) is the ethyl ester of p-Coumaric acid. p-Coumaric Acid is a common dietary polyphenol and also a potent immunosuppressive agent in treating autoimmune inflammatory diseases like rheumatoid arthritis.

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

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

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

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

ICILIN (AG-3-5) is a synthetic TRPM8 ion channel super-agonist.

CNX-774 is a highly specific, irreversible, and orally active BTK inhibitor (IC50<1 nM).

NIBR-0213 is a potent and selective competitive S1P1 antagonist with activity against experimental autoimmune encephalomyelitis. In the GTPγ35S assay, it has IC50 values ​​of 2.0 nM and 2.3 nM for human and rat S1P1, respectively.

Complement factor D-IN-2 is an inhibitor that reduces the excessive activation of Complement factor D.

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

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3).

TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

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.

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

Piclidenoson (CF-101), a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.

TASP0415914 is an orally potent inhibitor of phosphoinositide 3-kinase γ (PI3Kγ). T

CPYPP is an inhibitor of DOCK2-Rac1 interaction. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner(IC50 : 22.8 µM). CPYPP also inhibits DOCK180, DOCK5 and

(Rac)-Benpyrine is a potent and orally active inhibitor of TNF-α.