4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model[1].
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM[1].
IL-17 modulator 4 sulfate is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator[1].
Melrilimab (GSK 3772847) is an IgG2-kappa anti-IL1RL1/ST2/IL33R/DER4/FIT-1 monoclonal antibody. Melrilimab can be used for the research of asthma[1].
IFN-α Receptor Recognition Peptide 1 is a peptide of IFN-α associated with receptor interactions[1].
Valeryl salicylate is a potent and irreversible cyclooxygenase-1 (COX-1) inhibitor. Valeryl salicylate shows anti-inflammatory effect[1].
FR122047 (hydrochloride) is a selective and oral active inhibitor of COX-1 with an IC50 of 28 nM. FR122047 hydrochloride has antiplatelet, analgesic and anti-inflammatory effects in vivo[1][2][3].
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma[1][2].
Firocoxib-d4 (ML 1785713-d4) is the deuterium labeled Firocoxib. Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1].
Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
Novel potent and selective antagonist of human Complement C3a receptor
PD-1/PD-L1-IN-19 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-19 blocks PD-1/PD-L1 with the IC50 of 62.3 nM. PD-1/PD-L1-IN-19 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity[1][2][3].
N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method[1].
ODN M362, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 induces cancer cell apoptosis[1][2].
KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain[1].
TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
Dimethindene is a potent, selective histamine H1 antagonist. Dimethindene impairs cutaneous wound healing (WH). Dimethindene can block K+ currents[1][2].
Piceatannol 3'-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide (NO) synthase through inhibition of arginase activity with IC50s of 11.22 µM and 11.06 µM against arginase I and arginase II, respectively.
Afimetoran is a toll-like receptor antagonist, which can be used in the research of inflammatory and autoimmune diseases[1].
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro[1].
Factor B-IN-5 (Example 5 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.2 μM. Factor B-IN-5 can be used for the research of diseases related to inflammation and immunity[1].
TLR4 agonist-1 (compound 17a) is a potent agonist of Toll-like Receptor 4 (TLR4), and induces the generation of MIP-1β in RAW 264.7 and MM6 cells[1].
Tinoridine (Y-3642) is an orally active non-steroidal anti-inflammatory agent with potent antiperoxidative ability and radical scavenger activity. Tinoridine acts function by inhibiting COX enzyme, involves in hepatotoxicity inhibition. [1][2][3].
Eciskafusp alfa is a programmed cell death 1 (PDCD1, best known as PD-1) cis-targeted IL2v immunocytokine. Eciskafusp alfa preferentially targets antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells and differentiates them towards a novel population of better effectors. Eciskafusp alfa can be used for the research of cancer and chronic infections[1].
(-)-Catechin, isolated from green tea, is an isomer of Catechin having a trans 2S,3R configuration at the chiral center. Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
Meloxicam sodium is a non-steroidal anti-inflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1].