Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease[1].
Nitecapone (OR-462) is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor with gastroprotective and antioxidant properties. Nitecapone (OR-462) scavenges reactive oxygen and nitric radicals and prevents lipid peroxidation[1][2][3].
Doxofylline-d4 is the deuterium labeled Doxofylline. Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV[1][2].
GVLSNVIGYLKKLGTGALNAVLKQ is an antimicrobial peptide with 24-amino acid. GVLSNVIGYLKKLGTGALNAVLKQ can potentially form α-helix. GVLSNVIGYLKKLGTGALNAVLKQ (PGQ) has activity against Gram-negative, Gram-positive bacteria and the yeast Candida albicans[1].
4-(2-Hydroxy-1-methoxyethyl)-1,2-benzenediol is a phenylethanoid isolated from the stem bark of Syringa reticulate (Bl.) Hara (Oleaceae) with expectorant and antiasthmatic activity[1].
CL097, a potent TLR7/8 agonist, induces pro-inflammatory cytokines in macrophages[1]. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production[2].
6-Hydroxyrubiadin, a natural anthraquinone, may be a potential therapeutic candidate for the treatment of inflammation and inflammatory diseases[1].
Kakkalide is an isoflavone derived from the flowers of Pueraria lobata. Kakkalide ameliorates endothelial insulin resistance by suppressing reactive oxygen species (ROS)-associated inflammation[1].
IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.
B 9430 is a potent bradykinin B1/B2 receptor antagonist[1].
Tetracosane (ALKANE C24) is a natural product that can be found in Acrostichum aureum. Tetracosane hows cytotoxicity and induces Apoptosis. Tetracosane has the potential for the research of peptic ulcer[1].
D-Ribose-d-2 is the deuterium labeled D-Ribose. D-Ribose is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose is active in protein g
MIQ-N-succinate is a hapten with a four-carbon chain. MIQ-N-succinate consist of MIQ and succinic anhydride. MIQ-N-succinate has a carboxylic acid end group to attach to the lysine residues on the carrier proteins[1].
2-Pyridylethylamine is a histamine-1 (H1R) receptor agonist. 2-Pyridylethylamine can reduce the joint injury induced by formalin in rats. 2-Pyridylethylamine can be used to study the spinal cord release of neuropeptide (NPY) [1].
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research[1][2].
Cimpuciclib tosylate is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity[1].
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent[1][2][3].
RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC50 of 1 nM [1].
Vercirnon is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.
LY 3000328 is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.
LS-102 is a selective synoviolin inhibitor (Syvn1). LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of ~15 μM. LS-102 has the potential for rheumatoid arthritis treatment[1][2].
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and drug-sensitive (DS) M. tuberculosis[1].
DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role[1].
Aurantimycin A (Adipogen), a depsipeptide antibiotic, displays strong activity against Gram-positive bacteria. Aurantimycin A is a substrate of the LieAB transporter[1][2].
K-80001 is an RXRα-binder and COX-1/2 inhibitor, with IC50s of with an IC50 of 82.9μM, 3.4μM, 1.2μM for RXRα, COX-1 and COX-2, respectively[1].
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM[1][2].
Eflapegrastim is a humanized IgG4 monoclonal antibody, is also a granulocyte colony-stimulating factor (G-CSF). Eflapegrastim targets to G-CSF receptor (c-Fms). Eflapegrastim stimulates proliferation and differentiation of neutrophil progenitor cells and maintains stable numbers of mature and functional neutrophils. Eflapegrastim also shortens the duration of neutropenia[1].
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1].
Antimalarial agent 16 (Compound 4h) is a parasite inhibitor. Antimalarial agent 16 shows antimalarial activity, and can inhibit P. falciparum parasite growth (IC50=2.0 nM)[1].