Interleukin

Dupilumab (REGN-668) is a fully human monoclonal antibody targeting the alpha subunit of the interleukin-4 receptor, thereby inhibiting IL-4 and IL-13 signaling. As a systemic immunomodulator, it has demonstrated efficacy in improving atopic dermatitis.

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.

Anakinra (Raleukin) is a cytokine inactivator and interleukin 1 receptor antagonist that can be used to study secondary phagocytic lymphohistiocytosis and rheumatoid arthritis.

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].

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.

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.

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

Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA) analog and an agonist of TLR3 as well as retinoic acid-inducible gene I (RIG-I) and melanoma differentiation-associated protein 5 (MDA5). It can induce innate immune responses in mammals and serve as a vaccine adjuvant to enhance both innate and adaptive immunity, while modulating the tumor microenvironment and directly inducing apoptosis in cancer cells. Poly(I:C) is commonly used to establish acute respiratory distress syndrome (ARDS) animal models for studying immune responses and disease mechanisms.

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

Secukinumab is a fully humanized monoclonal anti-IL-17A antibody and the first in its class to be approved by the US Food and Drug Administration for the treatment of moderate to severe plaque psoriasis.

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.

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

1. Orientin (Luteolin-8-glucoside) may be regarded as a candidate therapeutic agent for treatment of vascular inflammatory diseases via inhibition of the HMGB1 signaling pathway. 2. Orientin protects vascular barrier integrity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases. 3. Orientin has neuroprotection effect by the intracellular mediation of caspase activity; may alleviate cognitive deficits and oxidative stress in AD mice; can exert antidepressant-like effects on CUMS mice, specifically by improving central oxidative stress, neurotransmission, and neuroplasticity.

Siltuximab(CNTO-328) is a monoclonal antibody with anti-tumor activity targeting IL-6 for the study of giant lymph node hyperplasia (MCD) and COVID-19.

Canakinumab (ACZ885) is a recombinant human IL-1β-targeting monoclonal antibody that inhibits human and chorioallantoic monkey IL-1β with IC50 values of 43.6 and 40.8 pM, respectively. It exhibits anti-inflammatory activity by neutralizing IL-1β signaling, and it has been used for the treatment of gout and coronary artery disease.

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.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A with a Kd value of <3 pM. It blocks the binding of IL-17A to IL-17RA but not to other IL-17 family members. Ixekizumab is used for the treatment of moderate to severe plaque psoriasis, psoriasis, arthritis, and psoriasis.

Spesolimab (BI 655130) is an anti-interleukin-36 receptor antibody. It plays a crucial role in the immune system by reducing biomarkers associated with congenital Th1/Th17 and neutrophil pathways. Spesolimab can be used to study systemic pustular psoriasis, palmar and plantar impetigo (PPP), and atopic dermatitis.

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.

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.

Astragaloside II (Astrasieversianin VIII) is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteogenic activities, differentiation, proliferation, and mineralization, through the bone morphogenetic protein-2/MAPK and Smad1/5/8 pathways.

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).

Tebentafusp (IMCgp100) is a protein that specifically targets gp100 and consists of a soluble T-cell receptor functionally fused to an anti-CD3 immune effector Tebentafusp has potential anti-tumor activity, induces the production of inflammatory cytokines and cytolytic proteins, and can be used to study unresectable or metastatic uveal melanoma.