IL-18 Inhibitor

Camoteskimab is a fully human monoclonal antibody with high affinity targeting IL-18. Camoteskimab is applicable to the research of autoinflammatory diseases.

ODN TTAGGG (ODN A151), an inhibitory oligonucleotide (ODN), is a TLR9, AIM2, and cGAS antagonist. ODN TTAGGG inhibits AIM2 inflammasome activation and cGAS activation through competition with DNA. ODN TTAGGG blocks AIM2-mediated Pyroptosis and inhibits IL-18 production. ODN TTAGGG has immunosuppressive effects and can be used in research on related autoimmune diseases such as lupus erythematosus. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.

LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia.

NP3-253 is an orally active and brain-penetranted NLRP3 inflammasome inhibitor. NP3-253 functions as a molecular glue that prevents NACHT-subdomain rearrangements, locking NLRP3 in an inactive conformation. NP3-253 inhibits production of pro-inflammatory cytokines IL-1β and IL-18. NP3-253 can be used for the research of inflammation and neurological disease, suah as peritonitis.

GSK-1070806 (Aletekitug) is a humanized IgG1/κ monoclonal antibody targeting IL-18. GSK-1070806 neutralizes IL-18 activity.GSK-1070806 can be used for the research of inflammation. The isotype control for GSK-1070806 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC₅₀ of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.

COM503 is a high-affinity anti-IL18BP human monoclonal antibody with a K_d value of 0.291 pM. COM503 binds to IL18BP, blocks the IL18BP:IL18 interaction, displaces IL18 from preformed complexes, and enhances the activation and function of T cells and NK cells. COM503 induces anti-tumor effects by relieving the activity inhibition of endogenous IL18 in the tumor microenvironment. COM503 can be used for cancer research. The recommended isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

MAS825 (Arumakimig) is a bispecific monoclonal antibody targeting IL-1β and IL-18. MAS825 reduces inflammatory infiltration and pulmonary alveolar proteinosis, and improves blood oxygen saturation, exercise tolerance and quality of life. MAS825 also promotes viral clearance. MAS825 can be used in research related to systemic juvenile idiopathic arthritis complicated with interstitial lung disease or macrophage activation syndrome, as well as COVID-19.

Sericin is an orally active globular protein produced by silkworm cocoons. Sericin inhibits the expression of COX2, iNOS, TLR4, MAPK and NF-κB; reduces the levels of IL-18, IL-1 and CCL2; antagonizes the activity of AChE; and downregulates the expression of Bcl-2. Sericin enhances the PI3K/AKT-mediated insulin signaling pathway. Sericin inhibits the activity of tyrosinase (Tyrosinase), scavenges ROS, chelates metal ions, and increases the levels of antioxidant enzymes. Sericin induces apoptosis and arrests the cell cycle. Sericin exhibits antibacterial, moisturizing, cardioprotective and anticoagulant properties. Sericin can be used in research related to type 2 diabetes, hyperlipidemia, obesity, Alzheimer's disease, colon cancer, peripheral nerve injury and ischemic myocardial infarction.

NLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC₅₀ of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis.

Relaxin H3 (human) TFA is a relaxin peptide with anti-inflammatory, anti-apoptotic, anti-pyroptotic, anti-migratory, protective and anti-fibrotic activities. Relaxin H3 (human) TFA acts on RXFP1 to generate cAMP and reduce the levels of ATP and ROS. Relaxin H3 (human) TFA inhibits renal inflammatory pyroptosis (pyroptosis), NLRP3 inflammasome activation, caspase-1 activation, IL-1β/IL-18 secretion, collagen synthesis, TGF-β1 signaling pathway, Smad2 phosphorylation, myofibroblast differentiation, TIMP expression, and HRMEC migration. Relaxin H3 (human) TFA activates AMPK, upregulates MFN2 expression, improves mitochondrial quality control and membrane potential, inhibits apoptosis (apoptosis) and pyroptosis, restores retinal ultrastructure, and reverses excessive left ventricular collagen expression. Relaxin H3 (human) TFA can be used in studies related to kidney stones, nephrocalcinosis, diabetic cardiomyopathy, fibrotic cardiomyopathy, and diabetic retinopathy.

GI-Y2 is an orally active, selective Gasdermin D (GSDMD) inhibitor (K_d = 36.0 μM) with anti-pyroptosis activity. GI-Y2 targets GSDMD, impairs membrane anchoring of GSDMD-NT, and blocks GSDMD‑dependent lipid binding and pore formation. GI-Y2 suppresses GSDMD‑dependent pyroptosis and inflammation, mitigates atherosclerosis and cardiac injury, boosts cell survival, and reduces IL‑1β/IL‑18 secretion. GI-Y2 can be used for the research of atherosclerosis and septic myocardial injury.

GSTO1-IN-6 is an allosteric and covalent GSTO1 inhibitor with an IC₅₀ of 457 nM. GSTO1-IN-6 markedly reduces Lipopolysaccharides (LPS) (HY-D1056)-induced IL-1β (IC₅₀ of 1.9 μM) and IL-18 (IC₅₀ of 10. μM) secretion in human monocyte-derived macrophages. GSTO1-IN-6 covalently modifies GSTO1-Cys32, inducing conformational changes and protein destabilization. GSTO1-IN-6 can be used for the research of inflammatory diseases.

ABT-546 (A-216546) is an orally active ET_A receptor antagonist, with K_i values of 0.46 nM and 13000 nM for human ET_A and ET_B receptors, respectively, and exhibits >25000-fold selectivity over the ET_B receptor. ABT-546 effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC₅₀ = 0.59 nM) and arachidonic acid release (IC₅₀ = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 can be used for research on abdominal aortic aneurysm.

ABT-546 (A-216546) hydrochloride is an orally active ET_A receptor antagonist, with K_i values of 0.46 nM and 13000 nM for human ET_A and ET_B receptors, respectively, and exhibits >25000-fold selectivity over the ET_B receptor. ABT-546 hydrochloride effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC₅₀ = 0.59 nM) and arachidonic acid release (IC₅₀ = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 hydrochloride crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 hydrochloride inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 hydrochloride can be used for research on abdominal aortic aneurysm.

MBL-1 is an orally active anti-inflammatory agent. MBL-1 can be isolated from the fermentation broth of Aspergillus sp. derived from gorgonians. MBL-1 inhibits the activity of the hCOX-2 protein with an IC₅₀ of 5.77 μM. MBL-1 reduces the production of key pro-inflammatory mediators such as NO, ROS, IL-1β and IL-18 by inhibiting the MAPK/NF-κB and NLRP3 signaling pathways. MBL-1 exerts a protective effect against DSS-induced colitis. MBL-1 can be used for the research of ulcerative colitis.

Relaxin H3 (human) is a relaxin peptide with anti-inflammatory, anti-apoptotic, anti-pyroptotic, anti-migratory, protective and anti-fibrotic activities. Relaxin H3 (human) acts on RXFP1 to generate cAMP and reduce the levels of ATP and ROS. Relaxin H3 (human) inhibits renal inflammatory pyroptosis (pyroptosis), NLRP3 inflammasome activation, caspase-1 activation, IL-1β/IL-18 secretion, collagen synthesis, TGF-β1 signaling pathway, Smad2 phosphorylation, myofibroblast differentiation, TIMP expression, and HRMEC migration. Relaxin H3 (human) activates AMPK, upregulates MFN2 expression, improves mitochondrial quality control and membrane potential, inhibits apoptosis (apoptosis) and pyroptosis, restores retinal ultrastructure, and reverses excessive left ventricular collagen expression. Relaxin H3 (human) can be used in studies related to kidney stones, nephrocalcinosis, diabetic cardiomyopathy, fibrotic cardiomyopathy, and diabetic retinopathy.

VRT-18858 (RU-36384), the active metabolite of Pralnacasan (HY-19676), is a potent interleukin-1β converting enzyme (ICE) inhibitor (K_i = 1.4 nM). VRT-18858 inhibits LPS (HY-D1056)-induced IL-1β release (IC₅₀ = 0.42 µM) and S. aureus Cowan-induced IL-1β and IL-18 release (IC₅₀=1.3 and 2.1 µM, respectively) in human peripheral blood mononuclear cells. VRT-18858 can be used for osteoarthritis research.

ZBP1 PROTAC-1 is a Z-DNA-binding protein 1 (ZBP1) PROTAC degrader with a DC₅₀ of 25.69 nM. ZBP1 PROTAC-1 consists of a DNA aptamer that specifically binds to ZBP1 and an E3 enzyme-recruiting moiety. ZBP1 PROTAC-1 combines the specificity and covalent binding ability of DNA aptamers with the PROTAC-mediated degradation function. By degrading ZBP1, ZBP1 PROTAC-1 inhibits the phosphorylation of RIPK3/MLKL to necrotic apoptosis and reduces the levels of proinflammatory cytokines (IL-18, IL-1β, IL-6, TNF-α, IFN-β). ZBP1 PROTAC-1 can be used in the research of viral pneumonia and influenza A H1N1 virus infection.

NEK7 degrader-5 is a NEK7 degrader. NEK7 degrader-5 inhibits the release of proinflammatory cytokines IL-1β and IL-18. NEK7 degrader-5 can be used for the research of inflammatory and tumor diseases.