Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2].
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].
ADU-S100 ammonium salt is an activator of stimulator of interferon genes (STING).
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate[1]. Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products[2]. A systemic acquired resistance (SAR) signal in tobacco[3]. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor[5].
Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation[1].
diABZI STING agonist-1 (Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.
Regaloside B is a phenylpropanoid isolated from Lilium longiflorum. Regaloside B can inhibit the expression of iNOS and COX-2, has anti-inflammatory activity[1][2].
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats[3][4][5].
Vesencumab (MNRP-1685A) is IG1 antibody against neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and prevents the subsequent coupling of NRP-1 to VEGFR-2. Vesencumab has anti-angiogenic and anti-neoplastic activities. Vesencumab can be used in the research of metastatic solid tumors, including ovarian cancer[1][2].
A potent TLR7 agonist with EC50 of 59 nM.
Manfidokimab (AK120) is an anti-interleukin 4 receptor alpha (IL-4Rα) IgG4 monoclonal antibody[1].
UC-1V150 is a specific TLR7 (Toll-like receptor) agonist that stimulates cellular immune responses and has anti-tumor activity. UC-1V150 can be used to synthesize ISAC (Immune-Stimulating Antibody Conjugates) molecule[1][2].
JAK2/STAT3-IN-1 (compound (S)-10a) is a potent GP130 inhibitor with an IC50 of 3.04 µM. JAK2/STAT3-IN-1 shows anti-tumor activity[1].
AMD-070 is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood[1][2][3].
BMS-1166 hydrochloride is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
ARG1-IN-1 is a human arginase 1 inhibitor with an IC50 of 29 nM.
O-Acetylschisantherin L (Acetylschisantherin L) is a natural lignan, which exhibits inhibitory effects on LPS-induced NO production in BV-2 cells with an IC50 of 23.1 μM[1].
Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).
3-Phenoxybenzaldehyde has weak complement classical pathway inhibition and hemolytic activity[1].
(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.
Cavrotolimod is an immunostimulatory spherical nucleic acid (SNA) modified with type B CpG oligonucleotides designed to agonize TLR9 and elicit immune responses useful in oncology applications.
Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi[1][2][3].
MyD88-IN-1 is a potent MyD88 inhibitor. MyD88-IN-1 inhibits the interaction of TLR4 and MyD88 and suppressed the NF-κB pathway. MyD88-IN-1 can be used in research of cancer and inflammatory[1].
Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs[1].
Tebotelimab (MGD-013) is a human IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity[1][2][3].
KTX-497 is an orally active IRAK4 degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology[1].
NLRP3-IN-5 is a NLRP3 inflammasome inhibitor (WO2016131098 (N-((4-chloro-2,6-dimethylphenyl)carbamoyl)-4-(2-hydroxypropan-2- l)furan-2-sulfonamide))[1].
PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease[1].