IL-13 Inhibitor

SM-17 is a human monoclonal antibody targeting IL-17RB. SM-17 binds to human IL-17RB, inhibits the dimerization of IL-17RA/IL-17RB, blocks IL-25-induced phosphorylation of ERK1/2 and STAT5, and suppresses Th2-mediated inflammatory responses. SM-17 inhibits the secretion of IL-5, IL-9, IL-13 and IL-4, impairs the proliferation/expansion of ILC2 and Th2 cells, and restores filaggrin expression. SM-17 reduces immune cell infiltration, epidermal hyperplasia, goblet cell hyperplasia, collagen deposition, ear swelling and scratching behavior in animal models. SM-17 can be used in research related to atopic dermatitis and allergic asthma.

JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC₅₀ values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC₅₀s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).

Zumilokibart (APG-777) is an anti-IL-13 IgG1κ type humanized antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zumilokibart can be used for the research of atopic dermatitis (AD).

Romilkimab (SAR156597) is a humanized IG antibody that specifically targets IL-4 and IL-13. Romilkimab can be used for the research of diffuse cutaneous systemic sclerosis.

TSLP modulator-1 (Compound 14O) is a potent TSLP signaling modulator. TSLP modulator-1 exhibits potent inhibition of CCL17 and IL-1β mRNA expression. TSLP modulator-1 attenuates the protein levels of IL-6, IL-4 and IL-13. TSLP modulator-1 significantly attenuates calcium influx. TSLP modulator-1 exerts anti-inflammatory effects. TSLP modulator-1 effectively alleviates pruritus and atopic dermatitis-like symptoms.

Abrezekimab (UCB4144; VR 942) is a humanized, high-affinity, neutralizing anti-human-IL-13 antibody fragment that binds to IL-13. Abrezekimab prevents IL-13 binding to the IL-13 Rα1 subunit. Abrezekimab can be used for the research of asthma.

IL13Rα2 D1 is an effective IL-13/IL13Rα2 signaling axis inhibitor. IL13Rα2 D1 can inhibit IL-13-induced cell adhesion, migration, invasion, and proliferation. IL13Rα2 D1 can inhibit FAK, Src, AKT, ERK1/2 phosphorylation, and MMP expression. IL13Rα2 D1 can be used for research on cancers such as colorectal cancer.

Ompekimig is an immunoglobulin monoclonal antibody that targets IL-4, IL-13, IL-33. Ompekimig shows potential for use in immune-mediated inflammatory diseases such as asthma and atopic dermatitis.

Solaprubart (STAR-0310) is a fully human IgG1 subtype monoclonal antibody targeting OX40 (CD134/TNFRSF4), with a K_d of 7.2 nM. By blocking the OX40/OX40L co-stimulatory signal, Solaprubart effectively inhibits cytokine release (IFN-γ, TNF-α, IL-5, IL-13) from activated effector T cells (Th1/Th2/Th17-associated). Solaprubart can be used in research related to moderate-to-severe atopic dermatitis.

GED 0507-34-Levo is an orally active PPARγ modulator. GED 0507-34-Levo downregulates the expression of TGF-β, Smad3, IL-13, and CTGF in the colon. GED 0507-34-Levo improves DSS-induced chronic colitis and fibrosis.

Keap1-Nrf2 PPI-IN-2 is a Keap1-Nrf2 PPI inhibitor with an EC₅₀ of 14.2 μM. Keap1-Nrf2 PPI-IN-2 covalently binds to Keap1 cysteine residues through its electrophilic itaconate moiety, disrupts the Keap1-Nrf2 protein-protein interaction, releases Nrf2, and promotes its nuclear translocation and antioxidant gene expression, thereby reducing ROS and inhibiting IL-13 production. Keap1-Nrf2 PPI-IN-2 can be used for research on atopic dermatitis.

Anti-IL-13 Antibody (C836) is a neutralizing monoclonal antibody targeting human IL-13. The Fab fragment of Anti-IL-13 Antibody (C836) is a heterodimer composed of heavy chains and light chains, each folded into variable and constant domains. Anti-IL-13 Antibody (C836) can be used for chronic inflammatory diseases, such as asthma.

PARP14 inhibitor 1 is an orally active, selective PARP14 inhibitor with an IC₅₀ of 5.52 nM. PARP14 inhibitor 1 exhibits favorable pharmacokinetic properties and in vivo safety. PARP14 inhibitor 1 enhances and stabilizes intracellular endogenous PARP14 protein levels, while effectively reducing the expression levels of IL-4, IL-13 and IL-17A. PARP14 inhibitor 1 can be used in research related to atopic dermatitis.

Anti-CD1a Antibody (OKT-6) is an anti-human CD1a IgG1 monoclonal antibody. Anti-CD1a Antibody (OKT-6) blocks T cell activation by blocking CD1a function. Anti-CD1a Antibody (OKT-6) can reduce the production of IFN-γ. Anti-CD1a Antibody (OKT-6) can be used for researches on cancer and inflammation such as leukemia. The recommend isotype control of Anti-CD1a Antibody (OKT-6): Mouse IgG1 kappa, Isotype Control (HY-P99977).

Envudeucitinibum (Envudeucitinib; ESK-001) hydrochloride is an orally active and selective TYK2 allosteric inhibitor with an IC₅₀ range of 104-149 nM. Envudeucitinibum hydrochloride blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum hydrochloride is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases.

MEDI-7836 is a humanized monoclonal antibody inhibitor that targets the interleukin-13 receptor. MEDI-7836 is promising for research of inflammation-related diseases.

PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC₅₀ of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC₅₀=4.04 nM), IL4 (IC₅₀=36.33 nM), IFNy (IC₅₀=2394 nM).

AVP-13358 is an orally active IgE inhibitor that effectively suppresses immunoglobulin E (IgE)-mediated immune responses, with IC₅₀ values of 8 and 3 nM for IgE inhibition in vivo and in vitro in BALB/c mice, respectively. AVP-13358 acts directly on T cells, inhibiting the production and release of IL-4, IL-5, and IL-13. It also targets other markers critical for the development of allergic responses, including the B cell IgE receptor (CD23) in human monocytes and the CD23 and IL-4 receptors in mouse B cells. AVP-13358 can be used in research related to anti-allergic responses.

GNE-7056 is an orally active interleukin-2-inducible T-cell kinase (ITK) inhibitor with a K_i of 0.2 nM against human kinase, and exhibits high selectivity over LCK kinase. GNE-7056 inhibits PLCγ-1 phosphorylation, suppresses the production of IL-2, IL-4, IL-13 and TH2 cytokines, reduces CD4⁺ T-cell proliferation, and inhibits activation-induced cell death of CD4⁺ T cells by decreasing the abundance of FasL. GNE-7056 can be used in asthma-related research.

CSL-360 is a chimeric unconjugated IgG1 monoclonal antibody targeting CD123. CSL-360 efficiently prevents the binding of IL-3 to CD123, abolishing IL-3 induced cell proliferation. CSL-360 can be used for acute myeloid leukemia (AML) research.