Zaloglanstat (ISC-27864) is the inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1), and can be used to study asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases, etc[1].
Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib[1].
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation[1].
Lefitolimod (MGN 1703) is a DNA-based TLR9 agonist and an immune surveillance reactivator. Lefitolimod induces HIV-specific immune responses and can be used for the research of cancer and HIV-1[1][4].
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM)[1][2].
Anti-Human IL-17A is a fully human anti-interleukin-17A monoclonal antibody. Anti-Human IL-17A can be used for research in psoriasis pathogenesis[1].
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O[1][2].
NLRP3-IN-20 (compound 11) is an orally available inhibitor of the NLRP3 inflammasome with an IC50 of 25 nM for IL-1β secretion. NLRP3-IN-20 has excellent pharmacokinetic properties and demonstrated significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis[1].
UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.
CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research[1][2][3].
RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases[1].
CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM)[1].
Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin[1][2].
IRAK4-IN-9 (compound 73) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-9 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer[1].
Cosibelimab (CK-301; TG-1501) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab has a functional Fc domain and is capable of inducing ADCC and complement-dependent cytotoxicity (CDC)-mediated killing of PD-L1+ cell lines, including lymphoma cells[1].
IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-10 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer[1].
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11[1].
STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells[1].
Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis[1].
Tozorakimab (MEDI-3506) is a human immunoglobulin G1 monoclonal antibody targeting interleukin-33. Tozorakimab can be used to research chronic obstructive pulmonary disease[1].
Ruzotolimod is the agonist of TLR7. Ruzotolimod has the potential for the research of HBV, COVID-19 or SARS-CoV-2 infection (extracted from patent WO2021130195A1)[1].
NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout[1].
BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively[1][2].
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).
Deracoxib-d3 is the deuterium labeled Deracoxib. Deracoxib, a selective cyclooxygenase-2 inhibitor, is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID).
Loxoprofenol-SRS tromethamine (HR1405-01), an active metabolite of Loxoprofen, is a Safe intravenous non-steroidal anti-inflammatory drug (NSAID) with superior anti-inflammatory and analgesic activities[1].
KP136 is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.
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].