TNF Receptor Inhibitor

SAP 2.8 peptide is an antimicrobial peptide. SAP 2.8 peptide induces bacterial membrane rupture and permeabilization, triggers an increase in intracellular ROS production, and causes bacterial death. SAP 2.8 peptide inhibits bacterial biofilm formation and disrupts established biofilms. SAP 2.8 peptide reduces bacterial load in animal models. SAP 2.8 peptide can be used for research on bacterial infections, skin and soft tissue infections, and peritonitis.

Anti-inflammatory agent 105 (Compound 12) is an anti-inflammatory compound. The IC₅₀ of Anti-inflammatory agent 105 for the inhibition of TNF-α synthesis and release in the human macrophage cell line U937 is 0.124 nM.

TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3 (HY-150758). TNF-α-IN-9 is a TNF-α inhibitor. TNF-α-IN-9 shows low inhibitory activity.

CAY10512 is a NF-κB inhibitor. CAY10512 can suppress the upregulation of NF-κB-sensitive proinflammatory miRNAs (miRNA-9, miRNA-125b, miRNA-146a, miRNA-155) in cerebrospinal fluid and extracellular fluid. CAY10512 significantly reduces the release of pro-inflammatory cytokines (such as TNF-α, MCP-1, IL-8, IL-6). CAY10512 can be used for researchs on neuroinflammation, islet transplantation and microRNA regulation.

Anti-inflammatory agent 118 is a bergenin derivative with anti-inflammatory activity. Anti-inflammatory agent 118 inhibits the expression of iNOS through negative feedback regulation mediated by NO release, while blocking the phosphorylation of p65 protein and reducing the secretion levels of two pro-inflammatory cytokines, TNF-α and IL-6. Anti-inflammatory agent 118 can be used for the research of inflammation-related diseases.

Immuno modulator-1 (compound 22) inhibits TNFα and IL-2 secretion in human peripheral blood mononuclear cells (hPBMC), with IC₅₀ values of 4.7 and 26 nM, respectively. Immuno modulator-1 shows hERG potassium channel blocking effect, with Inhibitory percentage of 20% at 3 μM.

Cloricromen (Cloricromene) is an orally active platelet inhibitor. Cloricromen inhibits thromboxane B₂ release, β-thromboglobulin, and thrombus formation. Cloricromen inhibits LPS (HY-D1056)-induced NF-κB activation, oxidative activity, and TNF-α expression. Cloricromen exhibits protective activity in animal models of shock and peripheral ischaemia. Cloricromen can be used for the research of myocardial ischaemia/reperfusion injury, and ischaemic cerebrovascular disease.

BC011 is a human monoclonal antibody (mAb) targeting TNFRSF1B. BC011 promotes CD8+T cell proliferation and depletes Treg cells, thereby increasing the proportion of effector T cells in the tumor microenvironment. BC011 can be used in tumor Immunity research.

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis.

Monoolein is a biocompatible lipid molecule that can be used as a carrier for bone repair. Monoolein exhibits anti-inflammatory activity by inhibiting the immune response induced by LPS (HY-D1056). It exerts its anti-inflammatory effects by reducing the production of immune response factors such as IL-12 p40, IL-6, and TNF-α, and inhibiting the generation of NO. Monoolein can be used in drug delivery and research in the field of inflammatory diseases .

Norketotifen is the active metabolite of Ketotifen (HY-B0157). Norketotifen exhibits skin anti-inflammatory activity, anti-malarial activity, and antipruritic activity against non-histamine-mediated dog itching in mice. Norketotifen effectively inhibits TNF-α release without causing any sedative side effects. Norketotifen can be used for research on non-sedating anti-inflammatory agents.

Sinulatumolin C (compound 3) is an anti-inflammatory agent. Sinulatumolin C has significant TNF-α inhibitory activity with an IC₅₀ value of 2.6 μM.

NMB04 is a recombinant anti-Human CD257 (BAFF) (BLyS) antibody. NMB04 binds with specificity and high affinity to soluble and membrane-bound Blys, and blocks Blys binding to receptors TACI, BCMA, and BR-3. NMB04 can be used for the research of autoimmune diseases.

Anhydro-Ouabain (compound 20) is a cardiotonic steroid which shows anti-inflammatory and neuroprotective activities and thus can be used in neurological research.

STING Degrader-3 is a PROTAC-like STING degrader with a DC₅₀ of 2.58 μM in THP-1 cells. STING Degrader-3 degrades STING protein via the lysosomal pathway. STING Degrader-3 functions as a non-degradative inhibitor in macrophages. STING Degrader-3 reduces the phosphorylation levels of TBK1 and IRF3, and downregulates the expression of IFN-β, CXCL10, IL-6, TNFα, IL-1β, ISG15 and ISG56. STING Degrader-3 exhibits renoprotective properties in a cisplatin-induced acute kidney injury model. STING Degrader-3 can be used in studies related to acute kidney injury. ((Pink: STING ligand (HY-168676); Blue: CRBN ligand (HY-126457); Black: linker (HY-W123015); CRBN ligand + linker: (HY-168677)).

Mitochonic acid 35 is an IAA analogue with cytoprotective effects.

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a K_i of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.

RIPK2-IN-7 (Compound 10w) is an orally active, selective RIPK2 inhibitor (IC₅₀: 0.6 nM). RIPK2-IN-7 inhibits RIPK2 kinase activity, blocks the nucleotide-binding oligomerization domain (NOD) signaling pathway, and reduces the production of inflammatory factors (such as TNFα). RIPK2-IN-7 can be used in the study of inflammatory bowel disease (IBD).

LMP-420 is a selective tumor necrosis factor-α (TNF-α) inhibitor. LMP-420 reduces the release of pro-inflammatory cytokines (e.g., IL-1β, IL-2), inducing the expression of anti-inflammatory cytokine IL-10 and anti-apoptotic molecules SOCS-1 and Mn-SOD. LMP-420 also downregulates chemokines (e.g., IP-10, MCP-1) to reduce immune cell infiltration. LMP-420 is promising for research of type 1 diabetes mellitus, inflammatory diseases (e.g., colitis), and HIV-Mycobacterium tuberculosis coinfection.

Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside is an anti-inflammatory agent. Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside exerts significant anti-inflammatory effects in LPS (HY-D1056)-induced RAW 264.7 macrophages by inhibiting the NF-κB, MAPK and Akt signaling pathways, thereby reducing the production of inflammatory mediators (NO, PGE2) and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6).