Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Polyinosinic-polycytidylic acid presents in some viruses, and is therefore commonly used to model the actions of extracellular dsRNA.
Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer[1][2].
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation. ADS032 can reduce NLPR1 and NLRP3 activation of human macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduce NLRP3-induced ASC speck formation. ADS032 protected mice against the deadly influenza A virus, reducing inflammation in the lungs and improving survival. ADS032 inhibits Nigericin (HY-127019)-induced IL-1β secretion with IC50s of 94.6 μM (No wash out) and 354 μM (Wash out) respectively[1].
Plerixafor is a selective CXCR4 antagonist with an IC50 of 44 nM.
Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1].
Ermanin is a flavonoid isolated from Tanacetum microphyllum. Ermanin potently inhibits iNOS, COX-2 activities, and inhibits platelet aggregation. Ermanin has anti-inflammatory, anti-tuberculous and anti-viral/bacterial properties[1][2].
STING agonist C11 is a novel cell-permeable STING agonist that activates IFN-dependent signaling processes and induces IFN secretion from human cells; induces transcription and translation of interferon-dependent antiviral genes, induces canonical IRF3 phosphorylation and ISG transcription in a manner that requires STING but not MAVS or TRIF; potently blocks replication of multiple emerging Alphavirus types including Chikungunya, Ross River, Mayaro, and O'nyong'nyong viruses.
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].
Iparomlimab is an anti-human PD-1/CD279/PDCD1 IgG4κ antibody. Iparomlimab also targets to human monoclonal PSB103 γ4-chain, disulfided with human monoclonal PSB103 κ-chain to form a dimer. Iparomlimab can be used for Oncology research[1].
AX-024 hydrochloride is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.
SCH 546738 is a novel, potent and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
Tralokinumab, a fully human IgG4 monoclonal antibody, specifically binds with high affinity to IL-13 alone, preventing its interaction with the receptor and subsequent downstream signalling. Tralokinumab can be used for the research of the atopic dermatitis (AD)[1].
Citrostadienol is a steroid compound with anti-inflammatory and anticomplementary activities. Citrostadienol demonstrates inhibition activities on classical complement pathway (IC50 of 46 nM)[1].
PD-1/PD-L1-IN-18 (Compound L31) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-18 blocks PD-1/PD-L1 with the IC50 of 1.054 μM. Antitumor Activity[1].
AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM[1]. AR-C102222 hydrochloride has antinociception and anti-inflammatory activities[2].
Durvalumab (MEDI 4736) is an humanized anti-PD-L1 monoclonal antibody. Durvalumab blocks the interaction of PD-L1 with PD-1 and CD80[1].
Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment[1][2].
Shegansu B is an inhibitor of IL-1β. Shegansu B 6 inhibits IL-1β expression on LPS-induced THP-1 cells with 64.74% inhibition. Shegansu B has anti-inflammatory activity[1].
PD-1/PD-L1-IN-30 is a PD-1/PD-L1 binding inhibitor, with an IC50 value of 0.018 μM. PD-1/PD-L1-IN-30 can be used for research of cancers and other related diseases[1].
AChE-IN-14 is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1].
Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis[1]. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities[1].
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis[1].PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].
Carlumab (CNTO 888) is a humanised anti-CCL2 (chemokine ligand 2) antibody with high affinity. Carlumab can be used in cancer research, particularly in prostate cancer[1].
ODN M326 (CpG-ODN M326) is a potent TLR9 agonist. ODN M326 induces the production of TNF. ODN M326 can be used as a vaccine adjuvant[1].
Phenylbutazone-d10 (diphenyl) is the deuterium labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research[1][2].
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages[1][2][3].
C-021 dihydrochloride is a potent and orally bioavailable CCR4 antagonist with IC50 of 0.14 uM and 0.039 uM for inhibition of chemotaxis in human and mouse, respectively.
Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor inhibitor with an IC50 of 0.1 nM.