Interleukin

Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

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

Y-320 is a new phenylpyrazoleanilide immunomodulator.

Ustekinumab is an anti-IL-12 IL-23 IgG1κ human monoclonal antibody.

Tocilizumab (Anti-Human IL6R) is a neutralizing antibody against human interleukin-6 receptor (IL-6R) that blocks the binding of IL-6 to IL-6R, thereby inhibiting both classical and trans signaling. It can be used to study rheumatoid arthritis and has been suggested as a possible drug for the treatment of severe COVID-19.

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15 1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

IL-17 modulator 4 is a prodrug of IL-17 modulator 1, which acts as a potent modulator of IL-17.

Cergutuzumab amunaleukin (CEA-IL2v) is a CEA-targeted IL-2 variant immunocytokine for combination cancer immunotherapy with immunostimulatory and anti-tumor activities for the study of solid cancers.

Vixarelimab (KPL-716) is a human anti-oncostatin M (OSM) monoclonal antibody with affinity for the beta chain of the OSM receptor, inhibiting IL-31 and OSM signaling. It can be used to study severe nodular itch and idiopathic pulmonary fibrosis.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

JAK2 STAT3-IN-1 is a GP130 inhibitor with anti-tumor effects and can be used to study inflammation, autoimmunity and cancer.

1. Negletein (7-O-Methylbaicalein) has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β. 2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. 3. Negletein shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. 4. Negletein shows significant antimicrobial activity. 5. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.6. Negletein has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. 7. Negletein (IC50: 3.89 + - 0.39 microM) exhibits potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor.

Nemolizumab (CIM331) is a humanized monoclonal antibody targeting the human interleukin-31 receptor A, inhibiting IL-31 binding and subsequent signal transduction. It is useful for studying atopic dermatitis with pruritus.

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.VU0285655-1 has an inhibitory effect on high glucose-induced caspase-3 cleavage and reduction of cell viability.VU0285655-1 is used in the study of diabetic retinopathy.

Astegolimab (RG 6149) is a humanised IgG2 monoclonal antibody that targets the IL-33 receptor and inhibits IL-33 signalling. Astegolimab is used in the study of chronic obstructive pulmonary disease (COPD) and severe asthma in adults.

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

1. Mulberroside has nephroprotective, hypoglycemic, and antidiabetic effects. 2. Mulberroside A is a glycosylated stilbene of oxyresveratrol; thus, the deglycosylation of Mulberroside A resulted in enhanced inhibition of melanogenesis. 3. Mulberroside A has anti-inflammatory antiapoptotic effects. by decreasing the expressions of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 and inhibiting the activation of NALP3, caspase-1, and nuclear factor-κB and the phosphorylation of extracellular signal-regulated protein kinases, the c-Jun N-terminal kinase, and p38.

SC144 is an orally active small-molecule gp130 inhibitor.

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

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

Ginsenoside Rh1 (Sanchinoside B2) , one of the main constituents of Panax ginseng, exhibits anti-inflammatory effect.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

Benralizumab (MEDI-563) is a monoclonal antibody targeting the interleukin-5 receptor alpha (IL-5Rα). It enhances antibody-dependent cell-mediated cytotoxicity, leading to a rapid depletion of eosinophils. Benralizumab is used for severe eosinophilic asthma and can be employed to prevent exacerbations of chronic obstructive pulmonary disease.

Kansuinine A possesses analgesic props, it also shows NGF inducing activity.

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) exhibits anti-inflammatory, antibacterial, and antifungal activities, along with moderate antitrypanosomal activity, having an MIC value of 19.0 µg mL.

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).

Hydrocortisone hemisuccinate (hydrocortisone 21-hemisuccinate*free acid) is a corticosteroid used as an analytical and chromatography reagent.

Fezakinumab is a potent monoclonal antibody to interleukin-22 (IL-22). Fezakinumab can be used to study immune system diseases and inflammation-related conditions such as psoriasis, rheumatoid arthritis and atopic dermatitis.

RCGD423, a small molecule gp130 modulator, prevents articular cartilage degeneration and promotes repair.

AX-024 hydrochloride (AX-024 HCl) is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.

APY0201 is a effective, highly specific, ATP-competitive PIKfyve inhibitor (IC50: 5.2 nM). It can interrupt the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3, 5)P2.

GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation.

RP-54745, a potential antirheumatic compound. Inhibitor of macrophage stimulation and interleukin-1 production.

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM and exhibits significant anti-inflammatory activity.

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).

Ginsenoside Rc (Panaxoside Rc) is one of the ginsenosides from Panax ginseng, inhibits the expression of TNF-α and IL-1β.

Oxelumab (R 4930) is a human monoclonal antibody targeting OX40L, and could be used to study asthma.

Methylthiouracil (NSC-193526) is a thiourea antithyroid agent that inhibits the synthesis of thyroid hormone, and it is used to treat hyperthyroidism.

Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6 GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.

Fibrinogen is a heterodimeric protein that can be cleaved by thrombin. Fibrinogen is a potential marker for cardiovascular disease and plays an important role in metabolism. Its absence can cause fibrinogenemia.

RO2959 Hydrochloride (RO2959 HCl) is a potent and selective inhibitor of CRAC channel(IC50: 402 nM). It is also a potent inhibitor of human IL-2.

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

Suplatast Tosilate (IPD 1151T) is a novel capsular anti-asthmatic drug with an IC50 above 100 μM, inhibiting both IgE production and the synthesis of IL-4 and IL-5.

NSC 247030 inhibits interleukin 2 (IL-2) production.

Deacetylasperulosidic Acid is a natural compound of Morinda citrifolia fruit. It has antioxidant activity by increasing superoxide dismutase activity. It also prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells.

Pectolinarin is a Cirsium isolate with anti-inflammatory activity.

Madecassic acid (L-fucopyranose) is extracted from the whole herb of Centella asiatica.