IL-12 Inhibitor

Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC₅₀ of 0.2 nM and a K_i of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.

Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC₅₀s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.

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

Briakinumab (ABT-874) is a fully human anti-IL-12/23p40 monoclonal antibody. Briakinumab targets and neutralizes IL-12 and IL-23. Briakinumab can be used for the research of rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis.

PTD-N5-1 is an IRF5 inhibitory peptide. PTD-N5-1 blocks the activation of IRF5. PTD-N5-1 inhibits β-glucan-induced IL-12 production in bone marrow-derived dendritic cells pre-stimulated with IFN-γ. PTD-N5-1 reduces the levels of IL-12 and IFN-γ in the kidneys of mice with Candida albicans infection. PTD-N5-1 is applicable to the research of Candida albicans infection.

Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC₅₀ of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease.

PTD-N5-1 acetate is an IRF5 inhibitory peptide. PTD-N5-1 acetate blocks the activation of IRF5. PTD-N5-1 acetate inhibits β-glucan-induced IL-12 production in bone marrow-derived dendritic cells pre-stimulated with IFN-γ. PTD-N5-1 acetate reduces the levels of IL-12 and IFN-γ in the kidneys of mice with Candida albicans infection. PTD-N5-1 acetate is applicable to the research of Candida albicans infection.

Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC₅₀s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.

APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P₂ in the presence of in the presence of [³³P]ATP with an IC₅₀ of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

Suciraslimab (SM03) is an anti-human CD22 monoclonal antibody. Suciraslimab inhibits NLRP3 and ASC signaling. Suciraslimab suppresses cytokine (IL-1β, IL-12, IL-23) secretion and α4 integrin expression. Suciraslimab improves working memory and neuroinflammation. Suciraslimab isotype control product: Human IgG1 kappa, Isotype Control (HY-P99001).

GlcNAc-MurNAc, a disaccharide, is a TLR4 agonist with a K_d of 383 μM for murine TLR4. GlcNAc-MurNAc directly binds to TLR4 and activates its downstream NF-κB and IRF pathways. GlcNAc-MurNAc improves Dextran sulfate sodium salt (DSS) (HY-116282C)-induced colitis in mice through a TLR4-dependent mechanism. GlcNAc-MurNAc can be used for the study of inflammatory bowel disease.

Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases.

Anti-IL-12 p70 Antibody (20C2) is an anti-human IL-12 p70 IgG1 monoclonal antibody. Anti-IL-12 p70 Antibody (20C2) can inhibit the production of IFN-γ. Anti-IL-12 p70 Antibody (20C2) can be used for research on inflammation conditions. The recommend isotype control of Anti-IL-12 p70 Antibody (20C2): Rat IgG1 kappa, Isotype Control (HY-P99979).

(+)-Medioresinol is a furofuran-type lignan with antifungal and antibacterial properties. (+)-Medioresinol synergizes with antibiotics to exert antimicrobial and antibiofilm effects. (+)-Medioresinol induces intracellular ROS accumulation and mitochondrial-mediated apoptosis in Candida albicans. (+)-Medioresinol inhibits LPS (HY-D1056)-stimulated IL-12p40 production. (+)-Medioresinol is a PGC-1α activator that protects against endothelial cell pyroptosis in ischemic stroke via the PPARα-GOT1 axis. (+)-Medioresinol can be used in research on fungal and bacterial infection, inflammation, and ischemic stroke.

QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC₅₀=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC₅₀=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE).

Pentadecane is an orally active natural plant volatile alkane with anti-inflammatory, analgesic, antipyretic and anti-leishmanial activities. Pentadecane presents IC₅₀ values of 65.3 μM, 60.5 μM and 194.8 μM against Leishmania infantum promastigotes, amastigotes and intracellular amastigotes, respectively. Pentadecane downregulates the mRNA expression of TNF-α and IL-12 and inhibits the release of inflammatory mediators. Pentadecane arrests the cell cycle of Leishmania infantum and induces apoptosis. Pentadecane can be applied to the research of inflammation and leishmaniasis.

Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.

Isomucronulatol 7-O-glucoside (Isomucronulatol 7-O-β-D-glucoside) is an isoflavonoid glycoside isolated from the roots of Astragalus membranaceus. Isomucronulatol 7-O-glucoside targets inflammation-related pathways in vitro to exert anti-inflammatory activity without cytotoxicity at effective concentrations. Isomucucronulatol 7-O-glucoside inhibits NO production and weakly suppresses IL‑12 p40 production in vitro. Isomucronulatol 7-O-glucoside can be used for the research on inflammation.

Pentadecane-d₃₂ is the deuterium labeled Pentadecane (HY-N7926). Pentadecane is an orally active natural plant volatile alkane with anti-inflammatory, analgesic, antipyretic and anti-leishmanial activities. Pentadecane presents IC₅₀ values of 65.3 μM, 60.5 μM and 194.8 μM against Leishmania infantum promastigotes, amastigotes and intracellular amastigotes, respectively. Pentadecane downregulates the mRNA expression of TNF-α and IL-12 and inhibits the release of inflammatory mediators. Pentadecane arrests the cell cycle of Leishmania infantum and induces apoptosis. Pentadecane can be applied to the research of inflammation and leishmaniasis.

BMS-279700 is an orally active Src-family kinase p56Lck inhibitor. BMS-279700 can block the production of proinflammatory cytokines (IL-2 and TNFα). BMS-279700 can inhibit T cell proliferation. BMS-279700 can be used for the researches of inflammation and immunology.