IFN-γ Antagonist 1 (AYCRDGKIGPPKLDIRKEEKQI) is an antagonist of interferon γ (IFN γ). IFN-γ Antagonist 1 inhibits IFN-γ induced HLR/DR antigen expression in Colon 205 cells with an IC50 value of approximately 35 μM. IFN-γ Antagonist 1 has potential applications in immune regulation[1].
Clematomandshurica saponins B shows significant inhibitory activity on cyclooxygenase-2 (IC50=2.58 mM)[1].
ODN D-SL03 is a C class CpG oligonucleotides, can induce stimulate PBMCs to produce high level of IFN-α. ODN D-SL03 can activate human B cells, NK cells and mononuclear cells and up-regulate expression of CD80, CD86 and HLA-DR on the surface of subsets in human PBMCs. ODN D-SL03 also can inhibit the growth of the tumor. ODN D-SL03 sequence: 5'-tcgcgaacgttcgccgcgttcgaacgcgg-3'[1].
Lodoxamide tromethamine (U 42585 E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2[1].
Serplulimab is humanized monoclonal anti-PD-1 antibody[1].
Dioxopromethazine is an orally active antihistamine. Dioxopromethazine inhibits asthmatic symptoms[1].
STING agonist-22 (CF501) is a potent non-nucleotide STING agonist. STING agonist-22 is a adjuvant by activating STING to induce the type I interferon (IFN-I) response and proinflammatory cytokine production. STING agonist-22 can be used as an adjuvant to boost the original protein vaccine, producing potent, broad, and long-term immune protection. STING agonist-22 can be used for SARS-CoV-2 variants and sarbecovirus diseases research[1].
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes[1].
Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.
γ-Tocopherol-d4 (D-γ-Tocopherol-d4) is the deuterium labeled γ-Tocopherol. γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity[1][2].
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
PROTAC IRAK4 degrader-8 (compound 2) is a PROTAC targeting to IRAK4 (IC50=15.5 nM)[1].
C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47)[1].
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
Guaiacol-d3 (2-Methoxyphenol-d3) is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
ST 2825 is a MyD88 dimerization inhibitor.
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for the treatment of asthma[1].
Sirukumab (CNTO-136) is a humanized monoclonal anti-IL6 (Interleukin Related) IgG1κ antibody. Sirukumab has the potential for active lupus nephritis research[1].
Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes[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].
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].
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase[1].
4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever[1][2][3]. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties[2].
Corydalmine (L-Corydalmine), an alkaloid isolated from roots of Corydalis Chaerophylla, inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].
STING-IN-7 (compound 21) is a potent STING inhibitor with an IC50 of 11.5 nM. STING-IN-7 inhibits the phosphorylation of STING and interferon regulatory factor 3 (IRF3)[1].
Oxyphenbutazone is a phenylbutazone derivative, with anti-inflammatory effect. Oxyphenbutazone is a non-selective COX inhibitor. Oxyphenbutazone selectively kills non-replicating Mycobaterium tuberculosis[1][2].
Retifanlimab is an anti-programmed cell death protein 1 (anti-PD-1) monoclonal antibody (mAb). Retifanlimab can be used for the research of gastroesophageal adenocarcinoma (GEA)[1].
AZD 1678 is a potent, selective orally bioavailable CCR4 receptor antagonist with pIC50 of 8.6 for hCCR4, pIC50 of 9.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.8. Asthma Phase 1 Clinical