3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity[1][2].
Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model[1].
C-178, a covalent inhibitor of STING, binds to Cys91, potently and selectively suppresses the STING responses elicited by distinct bona fide activators in mouse but not human. C-178 significantly reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity. C-178 blocks palmitoylation (PMA)-induced clustering of STING; inhibits the CMA-induced phosphorylation of TBK1 (downstream protein kinase of STING)[1].
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities[1].
Varokibart (TEV-53275) is a human IgG4λ antibody targeting IL5[1].
Danirixin is a selective, and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8.
ODN 24888 is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 involves in immune and inflammatory responses, can be used as a vaccine adjuvant[1][2].
seco-Isolariciresinol Diglucoside, a synthetic lignin, which is derived from the natural plant flaxseed. seco-Isolariciresinol Diglucoside reduces asbestos-induced NLRP3 expression, and NF-κB activation in macrophages (MF). seco-Isolariciresinol Diglucoside also activates Nrf2.
PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels.
Acapatamab (AMG-160) is a half-life extended bispecific T cell engager (HLE BiTE), including an anti-PSMA binding domain and an anti-CD3 binding domain with Kd values of 14.8 nM and 22.4 nM for hPSMA and hCD3, respectively. Acapatamab can be used in research of cancer[1].
Cadonilimab (AK104) is a targeting PD1/CTLA4 IgG1 scaffold Fc-engineered humanized antibody. Cadonilimab can be used for researching metastatic cervical cancer[1][2].
Mal-VC-PAB-(N-Me-amide-C3)-ADU-S100 triethylamine is an immune stimulator antibody conjugate (ISAC) comprising an anti-human epidermal growth factor receptor 2 (HER2) antibody, a STING agonist (ADU-S100) and a linker. Mal-VC-PAB-(N-Me-amide-C3)-ADU-S100 triethylamine can be uesd for cancer research (WO2018200812A1; example 5)[1].
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibit the interaction of hPD-1/hPD-L1[1].
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate[1].
C5a Anaphylatoxin (human) is a pro-inflammatory peptide and a leukocyte chemoattractant. C5a Anaphylatoxin (human) can be used to study inflammation and immunity, such as allergic asthma[1][2].
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis[1][2][3].
C29 is a Toll-like receptor 2 (TLR2) inhibitor.
Olokizumab (CDP 6038) is a humanized monoclonal antibody targeting the interleukin-6 (IL-6). Olokizumab can be used in research of rheumatoid arthritis (RA)[1].
GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD)[1].
Nofazinlimab (CS1003) is a humanised IgG4 anti-PD-1 monoclonal antibody. Nofazinlimab can be used for unresectable hepatocellular carcinoma (uHCC) research[1].
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine is a weak inhibitor of CYP2C19 and CYP2C9[1][2].
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitory activity against cyclooxygenase-1, with the IC50 value of 30.4 μM[1].
Flurbiprofen axetil is a non-selective cyclooxygenase (COX) inhibitor. Flurbiprofen axetil has anti-inflammatory effect[1].
Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model[1].
COX-2-IN-20 (Compound 5d) is a selective and orally active COX-2 inhibitor with an IC50 of 17.9 nM. COX-2-IN-20 shows anti-inflammatory activity[1].
MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively; also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM); elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.
DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
PROTAC IRAK4 degrader-6 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172[1].
hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.IC50 value: 12 nMTarget: hPGDSThe detailed information please refer to WO2011044307A1 and WO2010080563A2