(+)-Oxypeucedanin methanolate (compound 9) is a natural compound with inhibitory effect on prostaglandin E2 production[1].
Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator[1][2].
Zansecimab (LY-3127804) is an immunoglobulin G4-kappa, a monoclonal antibody against angiopoietin 2 (Ang 2). Zansecimab has potential applications in angiogenesis and immune regulation[1][2][3].
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature[1].
Penicillamine is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.Target: OthersPenicillamine(Cuprimine, Depen) is used as an antirheumatic and as a chelating agent in Wilson's disease and is a chelating agent recommended for the removal of excess copper in patients with Wilson's disease. From in vitro studies which indicate that one atom of copper combines with two molecules of penicillamine. Penicillamine also reduces excess cystine excretion in cystinuria. The mechanism of action of penicillamine in rheumatoid arthritis is unknown although it appears to suppress disease activity. Unlike cytotoxic immunosuppressants, penicillamine markedly lowers IgM rheumatoid factor but produces no significant depression in absolute levels of serum immunoglobulins. Also unlike cytotoxic immunosuppressants which act on both, penicillamine in vitro depresses T-cell activity but not B-cell activity [1-3].
Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity[1]. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer[2].
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare[1]. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis[2].
DDR1/2 inhibitor-2 (Example 31) is a DDR1/DDR2 inhibitor, with IC50 values less than 100 nM. DDR1/2 inhibitor-2 can be used for research of cancer and fibrotic diseases[1].
Episappanol is a natural compound isolated from Caesalpinia sappan heartwood with anti-inflammatory activity. Episappanol significantly inhibits the IL-6 and TNF-α secretion[1].
HPK1-IN-11 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-11 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 2)[1].
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].
TUL01101 is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. TUL01101 can be used for the research of rheumatoid arthritis[1].
(R)-Elexacaftor is an enantiomer of Elexacaftor (HY-111772). (R)-Elexacaftor is the Compound 37 from patent WO2018107100A1. (R)-Elexacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR), the EC50 for CFTR dF508 is 0.29 uM[1].
p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively[1].
Robenacoxib is a nonsteroidal anti-inflammatory and analgesic agent. Robenacoxib is a selective COX-2 inhibitor[1][2].
Cucurbitacin R is a cucurbitacin. Cucurbitacin R can be isolated from the roots of Cayaponia tayuya. Cucurbitacin R can be used for the research of pain and inflammation[1].
JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer[1].
Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML)[1].
Physcion-d3 (Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects[1][2][3].
Trabikibart (CSL311), a βc-specific, fully human monoclonal antibody, binds to a unique epitope that is specific to the cytokine-binding site of the human βc receptor. Trabikibart has picomolar binding affinity for the human βc receptor. Trabikibart is a potent inhibitor of the combined effects of IL-3, GM-CSF and IL-5 on the survival of eosinophils. Trabikibart has the potential for chronic inflammatory diseases research[1].
Dexamethasone is a glucocorticoid receptor agonist.
RR-SRC is a substrate for src-tyrosine-specific protein kinase[1].
Rubropunctatin, an orange azaphilone pigment, is isolated from the extracts of Monascus pilosus-fermented rice (red-mold rice). Rubropunctatin has anti-inflammatory, immunosuppressive and antioxidative effects, and also exhibits anti-tumor activity[1][2][3].
Notopterol is a coumarin extracted from N. incisum. Notopterol induces apoptosis and has antipyretic, analgesic and anti-inflammatory effects. Notopterol is used for acute myeloid leukemia (AML)[1].
Antibacterial agent 52 (example 18) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
PF-184 is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. PF-184 has anti-inflammatory effects[1].
MMP-9-IN-7 is a potent MMP9 inhibitor with an IC50 of 0.52 μM in proMMP9/MMP3 P126 activation assay. MMP-9-IN-7 is extracted from patent WO2012162468 (example 59), and can be used for MMP9/MMP13 mediated syndrome research[1].
Pegozafermin is a fibroblast growth factor FGF21 (HY-P7012) analog, which is an endogenous metabolic hormone and regulates energy expenditure and glucose and lipid metabolism. Pegozafermin decreases the level of triglyceride (TG), can be used for non-alcoholic steatohepatitis (NASH) and severe hypertriglyceridemia (SHTG)[1][2].
IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].