Interleukin

Tocilizumab (anti-IL-6R) is a humanized monoclonal antibody that binds to the interleukin-6 receptor

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

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

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.

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.

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

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

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

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.

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).

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.

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.

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).

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

SC144 is an orally active small-molecule gp130 inhibitor.

Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.

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

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

Talacotuzumab (JNJ 56022473) is an IgG1 fully humanized CD123 neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has a high affinity for CD123, CD32b c, CD16-158F and CD16-158V, with KD of 0.43 nM, 188 nM, 46 nM and 16.8 nM, respectively. Talacotuzumab inhibits IL-3 signaling in target cells by inhibiting IL-3 binding to CD123. Talacotuzumab induces mutations in the Fc region to increase affinity for CD16 (FCγriiia), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab inhibits leukemia cell growth in xenografted mouse models of acute myeloid leukemia (AML).

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

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.

Aspartyl-alanyl-diketopiperazine (DA-DKP) is a known immunomodulatory molecule from the N terminus of human albumin.

Basiliximab (CHI 621) is a chimeric mouse human IgG1 monoclonal recombinant antibody against the interleukin-2 receptor. Basiliximab has good immunosuppressive activity and can be used in the study of kidney transplantation.

YM-90709 is a new-type antagonist inhibiting the binding of interleukin-5 to the interleukin-5 receptor.

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

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

VGX-1027 (GIT 27) is an isoxazole compound with various immunomodulatory properties.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

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

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.

Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

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

Pectolinarin is a Cirsium isolate with anti-inflammatory activity.

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

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

BRD6989 is an analog of the natural product cortistatin A (dCA). Which inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM.

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

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.

Lipoxin A4 (LXA4) is a lipoxygenase-derived arachidonate-like mediator with anti-inflammatory properties.Lipoxin A4 attenuates MSU crystal-induced NLRP3 inflammasome activation through inhibition of Nrf2, and regulates M1/M2 macrophage polarization through the FPR2-IRF pathway.Lipoxin inhibits oxidative stress and inflammation.

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.

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

Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A with a Kd value of <3 pM.Ixekizumab 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. arthritis, and psoriasis.

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].

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

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

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.

Sodium Thiocyanate, one of the main sources of the thiocyanate anion, is used as a precursor for the synthesis of pharmaceuticals and other specialty chemicals.

Nemolizumab (CIM331) is a humanized monoclonal antibody against human interleukin-31 receptor A that inhibits the binding and subsequent signal transduction of interleukin-31 (IL-31) to its receptor. Nemolizumab can be used to study atopic dermatitis with pruritus.

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

Armillarisin A enhancing the role of macrophages, inhibiting bacteria growth, improving the protein metabolism, and regulating liver function.