IL-2-IN-1 is an IL-2 inhibitor with antiproliferative activity for the study of diseases caused by abnormalities in the immune system.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

IL-17A inhibitor 1 is a IL-17A inhibitor with IC50 of <9.45 nM in alphalisa assay. IL-17A inhibitor 1 inhibits HT-29 cells with IC50 of 9.3 nM.

IL-1β-IN-1, a cannabidiol derivative, acts as a potent inhibitor of IL-1β, exhibiting significant anti-inflammatory and pain relief properties [1].

IL-1β-IN-2, a cannabigerol derivative, serves as a potent inhibitor of IL-1β, exhibiting anti-inflammatory and pain-resolving properties [1].

IL-17 Modulator 1 (disodium) is a potent, orally active compound, known for its high efficacy in modulating IL-17. This compound is extensively utilized for researching various diseases such as psoriasis, ankylosing spondylitis, and psoriatic arthritis[1].

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

IL-17A antagonist 1 is an IL-17A antagonist for the study of interleukin-related inflammatory and immune diseases.

Anti-Mouse IL-1R Antibody is an IgG2b subclass inhibitor targeting the mouse IL-1 receptor, sourced from Armenian hamsters.

IL-17A modulator-1 is an effective inhibitor of IL-17A activity, exhibiting a pIC 50 value of 8.2. This compound holds great promise for studying diseases and disorders that involve the modulation of IL-17A, such as immune-related diseases, autoimmune pathologies, cancer, and neurodegenerative disorders.

Anti-Mouse IL-1a Antibody is an IgG1 subtype inhibitor specific to mouse IL-1a, derived from the Armenian Hamster.

Anti-Mouse IL-1b Antibody is an IgG inhibitor specific to mouse IL-1b, derived from an Armenian Hamster host.

IL-17 modulator 4 is a prodrug of IL-17 modulator 1 which is an efficacious modulator of IL-17.

Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

Belnacasan (VX-765) is an orally active IL-converting enzyme/caspase-1 inhibitor.

Apilimod mesylate (STA 5326 mesylate) is a potent IL-12/IL-23 inhibitor.

(-)-Epicatechin (Epicatechin) is an inhibitor of cyclooxygenase-1 (COX-1), inhibiting the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

BI-69A11 ((E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one) is a dual AKT and NFkB pathway inhibitor. It enhances the susceptibility of colon cancer cells to mda-7/IL-24-induced growth inhibition by targeting Akt.

Lupeol acetate, a derivative of Lupeol, inhibits the progression of rheumatoid arthritis by downregulating TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.

AF 12198 Acetate is a novel low molecular weight antagonist of IL-1

K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.

(R)-Lisofylline ((R)-Lisophylline) is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 µM). (R)-Lisofylline interrupts IL-12 signaling-mediated STAT4 activation and can be used in studies about the treatment of type 1 diabetes and autoimmune disorders.

NMI 8739 (n-docosahexaenoyl dopamine) is an agonist of D2 autoreceptor. NMI 8739 reduces NO production and elicits concentration-dependent suppression of CCL-20, MCP-1 and IL-6 release.

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with IC50 of 574 nM. NLRP3-IN-NBC6 acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin -induced inflammasome activation in THP-1 cells and Imiquimod -induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation ( IC 50 =1 μM), does not blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

Pyrrolidinedithiocarbamate ammonium (1-Pyrrolidinedithiocarboxylic acid ammonium salt), a selective NF-κB inhibitor, inhibits translation of nitric oxide synthase mRNA to prevent induction.

T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.

CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.

STAMBP-IN-1 is a novel selective antagonist of deubiquitinase STAM-binding protein (STAMBP), decreasing NALP7 protein levels and suppressing IL-1β release after TLR agonism.

Cordycepin (3'-Deoxyadenosine) is a purine nucleoside antimetabolite and antibiotic isolated from the fungus Cordyceps militaris with potential antineoplastic activity.

Ginsenoside-F3 has immunoenhancing activity by regulating production and gene expression of type 1, type 2 cytokines in murine spleen cells. Ginsenoside-F3 enhances the NF-kappaB DNA binding activity induced by ConA in murine spleen cells (10 μM).

Lysicamine shows significant antioxidant capacity in the ORAC(FL) assay and it is active against S. epidermidis and C. dubliniensis, with MIC values in the range 12.5-100 microg mL(-1). Lysicamine has antimicrobial and anti-inflammation activity, the mini

Romilkimab (SAR156597) is a chimeric humanized immunoglobulin (Ig) antibody designed to specifically target interleukins 4 and 13 (IL-4 and IL-13) [1].

Stapokibart (CM310), a humanized monoclonal antibody, selectively binds to IL-4Rα, inhibiting the cytokines IL-4 and IL-13 from interacting with their shared co-receptor subunit, IL-4Rα. This compound demonstrates cross-species reactivity by interacting with IL-4Rα in humans, cynomolgus monkeys, and rats [1].

Lysophosphatidylcholine C19:0 (1-Nonadecanoyl-2-hydroxy-sn-glycero-3-phosphocholine), an acyl chain lipid, enhances IL-1beta secretion [1].

ATUX-1215, a protein phosphatase 2A (PP2A) activator, diminishes the phosphorylation of ERK, p38, JNK, and Akt, as well as decreases the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals, potentially decelerating lung fibrosis progression [1].

1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

MyD88-IN-1 is a potent MyD88 inhibitor MyD88-IN-1 has anti-inflammatory activity and inhibits downstream inflammatory signaling pathways, including the NF-κB pathway, of members of the Toll-like receptor (TLR) and interleukin-1 (IL-1) receptor family MyD88-IN-1 may be used for the study of cancer and the treatment of inflammation.

EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.

Avizakimab (BOS161721), a humanized IgG1 monoclonal antibody, specifically targets interleukin-21 [1].

JC2-11 is an inhibitory compound for inflammation.JC2-11 inhibits the recruitment domain-containing proteins NLRC 4, atypical in melanoma 2 (AIM 2) and atypical (NC) inflammatory vesicles by disrupting reactive oxygen species (ROS) production and caspase-1 activity.JC2-11 reduces caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) activity in inflammatory vesicles. JC2-11 reduced caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) release from inflammatory vesicles.

β5i-IN-1 is a selective inhibitor of β5i, exhibiting potent activity with an IC50 of 8.463 nM. It modulates immune responses by promoting the release of TNF-α and IL-6 and affecting NF-κB transcriptional activity. This compound has applications in the research of idiopathic pulmonary fibrosis [1].

Dectrekumab (QAX576), a humanized monoclonal antibody targeting IL-13, significantly reduces intraepithelial esophageal eosinophil counts and normalizes dysregulated esophageal disease-related transcripts in Eosinophilic esophagitis (EoE), offering sustained benefits. It is valuable for inflammation and immunology research [1].

Vopikitug, a human IgG1-kappa monoclonal antibody targeting the IL2RA (interleukin 2 receptor alpha subunit, IL-2RA, TAC, p55, CD25), exhibits antineoplastic activity [1].

NLRP3 agonist 1 (compound 23) serves as a potent, orally active agent that activates Caspase-1 enzyme, leading to the cleavage of proinflammatory cytokines pro-IL-1β and pro-IL-18 into their active forms [1].

QS-21, an immunostimulatory saponin, is a powerful vaccine adjuvant that stimulates both Th2 humoral and Th1 cell-mediated immune responses by interacting with antigen presenting cells (APCs) and T cells. Additionally, QS-21 activates the NLRP3 inflammasome, leading to the release of cytokines IL-1β and IL-18, which are dependent on caspase-1.

Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels. It also attenuates phosphor-STAT3 levels through the STAT3/SOCS3 signaling pathway [1].

Anti-inflammatory agent 58 exhibits IL-1β inhibition with an IC50 value of 1.08 μM and suppresses pro-inflammatory gene expression, protein secretion, and NF-κB phosphorylation [1].