il-15

IL-15-IN-1 is a selective and potent Interleukin 15 (IL-15) inhibitor, effectively inhibiting the proliferation of IL-15-dependent cells (IC50: 0.8 μM).

Ordesekimab (AMG 714) is a human IgG1 κ-anti-IL-15 (Interleukin Related) monoclonal antibody. Ordesekimab binds competitively to IL-15, inhibiting the interaction of IL-15 with the common gamma chain of the IL-2Rβ and IL-15 receptor complex, but not with the IL-15Rα chain. Ordesekimab can be used to study non-reactive celiac disease (NRCD).

Anti-IL-15 Antibody (DISC0280) is a human-derived antibody produced in CHO cells, targeting IL-15. It features a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 145 kDa. For its isotype control, refer to HumanIgG1kappa, Isotype Control.

Anti-Mouse IL-15 Antibody (AIO.3) is a rat-derived IgG2a, λ antibody inhibitor targeting mouse IL-15.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

COX-2/15-LOX-IN-6 (Compound 5l) is a dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.201 μM and 11.723 μM, respectively. In serum, it suppresses the expression of PGE, TNF-α, IL-6, and iNOS, and demonstrates anti-inflammatory activity in a carrageenan-induced rat edema model.

NEK7-IN-1 (Compound I-15) is an inhibitor of NIMA-related kinase 7 (NEK7) with an IC50 of less than 100 nM. It also effectively inhibits the release of IL-1β, exhibiting an IC50 of less than 50 nM.

NLRP3 IN 70 (compound 15) exhibited the potent NLRP3 inhibitory activity, effectively suppressing IL-1β secretion in THP-1 (IC50 = 23 nM).

PROTAC BTK Degrader-13 (Compound 25) is a targeted BTK PROTAC degrader with a DC50 of 0.27 μM. It inhibits BTK activity with an IC50 of 0.44 μM and suppresses IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. This compound also inhibits the p38 MAPK signaling pathway, thereby blocking the activation of the BCR (B cell receptor) signaling pathway. [Pink: ligand for target protein BTK ligand 15; Black: linker; Blue: ligand for E3 ligase cereblon]

15-LOX-IN-2 (Compound 2a) is an orally active inhibitor of COX-2/15-LOX and a partial agonist of PPARγ. It exhibits anti-inflammatory activity by inhibiting levels of 20-HETE, IL-1β, and TNF-α in LPS-treated RAW 264.7 cells. Additionally, it significantly enhances glucose uptake without the presence of insulin and is applicable in metabolic disease research.

NF-κB-IN-15 (compound 14r) is a potent NF-κB inhibitor. It reduces NO levels in LPS-stimulated cells and suppresses the release of IL-6, TNF-α, and IL-1β. Additionally, it hinders LPS-induced p65 phosphorylation and IκBα degradation. NF-κB-IN-15 exhibits anti-inflammatory properties and holds potential for research in acute lung injury (ALI).

β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-4 induces IL-31 production by human peripheral blood-derived mast cells in vitro when used at a concentration of 10 μg/ml and by rat mast cells in vivo following a 500 ng intradermal dose. It also inhibits growth of E. coli, P. aeruginosa, and S. aureus with lethal concentration (LC) values of 5, 12, and 15 μM, respectively, of S. carnosus (MIC = 4.5 μg/ml), and of C. albicans with a minimum fungicidal concentration (MFC) value of 7.5 μM.

(±)14-HDHA is a hydroxydocosahexaenoic acid, an oxidized metabolite of DHA generated intracellularly by enzymatic or non-enzymatic reactions, is one of the specific substrates of 15-PGDH and can be further oxidized to the anti-inflammatory 14-oxoDHA, and in primary alveolar macrophages, 14-HDoHE itself significantly inhibits LPS-induced IL-6 mRNA expression in primary alveolar macrophages, which may be relevant to inflammatory diseases such as asthma.

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM and an IC50 value of 0.109 μM. It tightly binds to TNF-α, blocking its interaction with TNFR1, and has potential for TNF-α mediated inflammatory and autoimmune disease research [1].

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.

13(S)-HpODE, a metabolite present in potato and Homo sapiens, is the (S)-enantiomer of 13-HpODE, a fatty acid containing a peroxy group, IL-13/13(S)HpODE stimulates MAO-A-mediated intracellular ROS generation and induction of p53 as well as p21 during apoptosis of A549 cancer cells and promotes apoptosis of HCT116 and CCF52 cells by upregulating p53 and p21 expression promoted apoptosis in HCT116 and CCF52 cells, constituting the IL-13 > 15-LO > 13(S)HpODE > PPARγ > MAO-A > ROS > p53 > p21 axis.

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial agent used in tuberculosis (TB) research, inhibiting the growth of Mtb H37Rv and M299 with MIC50 values of 2.3 and 7.8 μM, respectively. This compound also suppresses the expression of iNOS, thereby inhibiting NO, TNF-α, and IL-1β production [1].

β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg/ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg/ml, respectively) but not HepG2 or A549 cells (IC50s = 36.41 and 41.51 µg/ml, respectively). It also inhibits cAMP phosphodiesterase with an IC50 value of 96 µM.

NLRP3-IN-15 is a potent, selective inhibitor of the NLRP3 inflammasome, demonstrating efficacy by inhibiting IL-1β (interleukin-1 beta) release with an IC50 value of 0.114 μM. This compound is utilized in the research of inflammation.

JAK-IN-24, a JAK inhibitor, exhibits IC50 values of 0.534 nM and 24 nM in the presence of 4 μM and 1 mM ATP, respectively. Additionally, it effectively inhibits STAT5 phosphorylation induced by PBMC IL-15 with an IC50 of 86.171 nM.

STING agonist-24 (CF504), a non-nucleotide small-molecule STING agonist, activates STING, leading to increased phosphorylation of STING, TBK1, and IRF3. It elevates levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells, demonstrating activity against SARS-CoV series strains [1].

STING agonist-23 (CF505) is a non-nucleotide, small-molecule compound that stimulates STING, enhancing the phosphorylation of STING, TBK1, and IRF3. It elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells and demonstrates efficacy against SARS-CoV strains [1].

STING agonist-23 (CF508), a non-nucleotide small-molecule STING agonist, activates STING, thereby enhancing the phosphorylation of STING, TBK1, and IRF3. This activation elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Moreover, STING agonist-23 demonstrates efficacy against SARS-CoV series strains [1].