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

IL-17A modulator-2, exhibits inhibitory properties towards IL-17A, with a pIC50 of 8.3. Its effectiveness lies in attenuating the biological effects associated with IL-17A activity. IL-17A modulator-2 finds utility in the study of diseases and disorders characterized by dysregulated IL-17A modulation, such as those involving immune dysfunction, autoimmune pathology, cancer, and neurodegenerative conditions.

IL-17A inhibitor 2 is an IL-17A inhibitor for treating psoriasis, rheumatoid arthritis, and multiple sclerosis.

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.

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

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.

12R-LOX-IN-2 is an inhibitor of 12R-lipoxygenase (12R-LOX).12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and inhibits colony formation.12R-LOX-IN-2 also decreases the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 may be useful in the study of psoriasis and other skin-associated inflammatory diseases.

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.

Peldesine (BCX 34) is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.

Itaconate-alkyne (ITalk) is a bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of itaconate in inflammatory macrophages and enables biochemical evaluation and proteomic analysis of its direct targets.

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].

Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

1. Berberrubine chloride (9-Berberoline Chloride) has antitumor activity. 2. Berberrubine has antidiabetic activity. 3. Berberrubine dose-dependently inhibits IL-8 and MCP-1 protein levels in the media and mRNA expression of the cells stimulated with IL-1beta or TNF-alpha.

BD750 is an effective immunosuppressant and a JAK3 STAT5 inhibitor, inhibits IL-2-induced JAK3 STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM in mouse and human T cells, respectively)

Sphondin has anticonvulsant, anti-inflammatory, and anti-proliferative activities, it possessed an inhibitory effect on IL-1beta-induced increase in the level of COX-2 protein and PGE(2) release in A549 cells.

Neochlorogenic acid (trans-5-O-Caffeoylquinic acid) is an antioxidant compound used in the treatment of oxidative stress and related afflictions.

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).

Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug/ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.

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

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)

Fenamic acid (N-Phenylanthranilic acid) is a chloride channel blocker that causes renal papillary necrosis in rats. Fenamic acid serves as a parent structure for several nonsteroidal anti-inflammatory drugs (NSAIDs), including flufenamic acid, tolfenamic acid, mefenamic acid, and meclofenamic acid.

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

Simlukafusp alfa (FAP-IL2v) is an immunocytokine that consists of an antibody targeting fibroblast activation protein α (FAPα) linked to a variant of IL-2, which specifically interacts with IL-2Rβγ. The compound is of the human IgG1 isotype [1].

CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling.

K-14585 is a proteinase-activated receptor 2 antagonist. K-14585 inhibited PAR(2)-mediated p65 NFkappaB phosphorylation and NFkappaB-DNA binding. K-14585 inhibited SLIGKV-stimulated IL-8 production, but given alone increased IL-8.

Elsilimomab (B-E8), an IgG1 monoclonal antibody targeting interleukin-6 (IL-6), exhibits a dissociation constant (K D) of 22 pM and an inhibitory concentration (IC 50) of 1.4 nM. It is applicable in researching multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA) [1] [2] [3].

Quin C1 is a selective and potent formylpeptide receptor 2 (FPR2/ALX) agonist with anti-inflammatory activity, inhibits neutrophil and lymphocyte production in BALF, and reduces the expression of TNF-α, IL-1β, KC, and TGF-β1.Quin C1 is used in the study of lung injury.

Lenalidomide (sodium), a Thalidomide derivative, serves as a molecular glue and an orally active immunomodulator. It acts as a cereblon (CRBN) ligand and triggers selective ubiquitination and subsequent degradation of the lymphoid transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase. Echoing its specificity, Lenalidomide (sodium) inhibits the proliferation of mature B-cell lymphomas, notably multiple myeloma, and promotes IL-2 secretion from T cells [1] [2].

Drotrecogin alfa (activated) (DrotAA), a recombinant human activated protein C (APC), mitigates smoke-induced elevations in pulmonary microvascular permeability and proinflammatory cytokine IL-1β levels in rats. It also inhibits coagulation and inflammation while enhancing fibrinolysis. Drotrecogin alfa (activated) is applicable in severe sepsis research [1] [2].

Skullcapflavone I has anti-inflammatory and anti-allergic potential, it can significantly inhibit LPS stimulated NO and PGE(2) release in J774A.1 macrophages and inhibit LPS induced IL-6 production in a concentration dependent manner. Skullcapflavone I se

Ganglioside GT1b is a trisialoganglioside that is characterized by having two sialic residues linked to the inner galactose unit. It binds to the neurotoxins botulinum toxin serotype A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively.[1] Ganglioside GT1b-containing liposomes bind to the major coat protein VP1 from Merkel cell polyomavirus (MCPyV), which has been identified in Merkel cell carcinomas, identifying ganglioside GT1b as a putative MCPyV receptor. [2] Ganglioside GT1b decreases production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMCs) by 31.4, 30.5, 60, 59.5, and 58%, respectively, when used at a concentration of 10 μM [3] . Ganglioside GT1b mixture contains ganglioside GT1b molecular species with C18:1 and C20:1 sphingoid backbones.

Lauric acid-13C is intended for use as an internal standard for the quantification of lauric acid by GC- or LC-MS. Lauric acid is a medium-chain saturated fatty acid. It has been found at high levels in coconut oil.1Lauric acid induces the activation of NF-κB and the expression of COX-2, inducible nitric oxide synthase (iNOS), and IL-1α in RAW 264.7 cells when used at a concentration of 25 μM.2

Daclizumab (Zenapax) is a humanized monoclonal antibody that specifically inhibits the alpha subunit of IL-2R-HA. Daclizumab (Zenapax) can inhibit the binding of IL-2 and IL-2R-HA through specific binding to CD25. Daclizumab (Zenapax) studies multiple sclerosis.

Denileukin diftitox (DAB 389IL-2), a fusion protein toxin combining diphtheria toxin (DT) and interleukin 2 (IL-2), selectively depletes cells with the high-affinity IL-2 receptor (IL-2R), specifically CD25. By binding to these cells, it introduces diphtheria toxin to inhibit protein synthesis, leading to cell depletion [1] [2] [3].

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5

Gevokizumab, a powerful anti-IL-1β antibody, inhibits IL-1β signaling allosterically, effectively reducing IL-1β's binding affinity for its IL-1 receptor type I (IL-1RI) signaling receptor, while not affecting its interaction with the IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) [1] [2].

Efavaleukin alfa (AMG592) is a human monoclonal antibody comprising the IGHG1 Fc fragment fused to interleukin-2 (IL-2). It is typically expressed in Chinese Hamster Ovary (CHO) cells [1].

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-2 microglia stimulated by LPS and decreases LPS-induced cytotoxicity when used at concentrations ranging from 5 to 10 μM. It also decreases nitrite production when used at a concentration of 7.5 μM, an effect that can be partially reversed by the CB2 receptor antagonist AM630 and the PPARγ antagonist GW 9662 . (±)19(20)-EDP ethanolamide induces vasodilation of isolated preconstricted bovine coronary arteries (ED50 = 1.9 μM) and reduces tube formation by human microvascular endothelial cells (HMVECs) in a Matrigel assay.

Resolvins are a group of polyhydroxylated metabolites of docosahexaenoic acid (DHA) found in the inflammatory exudates of aspirin-treated experimental animals. 17(R)-HDHA is the primary oxygenation product of DHA when exposed to aspirin-inhibited cyclooxygenase-2. 17(R)-HDHA serves as a precursor to resolvins and has intrinsic biological activity, such as the inhibition of TNFα-induced IL-1β expression in human glioma cells.

IRAK-4 protein kinase inhibitor 2 is a potent interleukin-1 receptor-associated kinase-4 (IRAK-4) inhibitor(IC50 = 4 μM).

Clazakizumab, a monoclonal antibody, demonstrates high affinity and specificity towards the interleukin-6 (IL-6) cytokine, potentially inhibiting the cytokine response in COVID-19 caused by SARS-CoV-2. It is also under research for treating psoriatic arthritis (PsA) and renal antibody-mediated rejection [1] [2].

C 101248 is a selective and potent inhibitor targeting both mouse and human tandem pore domain halothane-inhibited K+ channel 1 (THIK-1, IC50= 50 nM), without affecting the K2P family members (TREK-1, TWIK-2) and Kv2.1. This compound effectively blocks tonic and ATP-evoked THIK-1 K+ currents as observed in whole-cell patch-clamp recordings of mouse hippocampal microglia. Additionally, C 101248 mitigates neuroinflammation by inhibiting the NLRP3-dependent release of IL-1β in isolated microglia.

Depemokimab (GSK-3511294) is a long-acting monoclonal antibody targeting IL-15, utilized in asthma research [1] [2].

Anrukinzumab (IMA-638), a humanized anti-IL-13 monoclonal antibody, effectively reduces lung inflammation in cynomolgus monkeys and shows potential in the studies of ulcerative colitis (UC) and asthma [1] [2] [3].

TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.