IL-5 Inhibitor

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.

Pyrrothiogatain is a transcription factor GATA3 inhibitor with an IC₅₀ of 54.7 μM. Pyrrothiogatain inhibits the DNA-binding activity of GATA3 and inhibits the T helper 2 (Th2) cell differentiation and expression of Th2 cytokines. Pyrrothiogatain shows anti-infection effect by inhibiting ACE2 expression. Pyrrothiogatain can be used for the researches of inflammation, immunology, infection and cancer, such as colon cancer and SARS-CoV-2 infection.

Verekitug (ASP-7266; TRAB-1; UPB-101) is a human monoclonal antibody targeting the thymic stromal lymphopoietin receptor (TSLPR), with a mean half-life of approximately 20 days. At doses of Verekitug ≥100 mg, complete and sustained TSLPR-specific occupancy is achieved, and the antibody does not bind to IL-7Rα. By inhibiting TSLP-driven inflammatory responses, Verekitug blocks TSLP-induced cell proliferation and TARC expression, while reducing fractional exhaled NO levels, blood eosinophil counts, and levels of IL-5 and IgE. Verekitug significantly improves scores for nasal polyps, nasal congestion and olfactory dysfunction, with favorable safety and good tolerability; potential adverse reactions include headache, upper respiratory tract infection, sinusitis and nasopharyngitis. Verekitug is used in relevant studies on asthma, chronic rhinosinusitis with nasal polyps and chronic obstructive pulmonary disease.

Bivalirudin, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin can be used for the research of thrombotic diseases and others.

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.

ANB032 is a human IgG4 kappa BTLA agonist monoclonal antibody. ANB032 inhibits activated T cell proliferation and reduces secretion of inflammatory cytokines. ANB032 can be used for the research of atopic dermatitis[1].

YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).YM-90709 potently inhibits the binding of [¹²⁵I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells with IC₅₀ values of 1.0 and 0.57 μM.

Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used for severe eosinophilic asthma.

Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticum collagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma.

Bivalirudin TFA, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin TFA inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin TFA also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin TFA can be used for the research of thrombotic diseases and others.

Gypenoside A is an orally active triterpenoid compound that can be isolated from Gynostemma pentaphyllum. Gypenoside A has anti-inflammatory and antioxidant activities. Gypenoside A also has a certain protective effect on cardiomyocytes and can inhibit apoptosis. Gypenoside A can be used in the research of cardiovascular diseases and inflammation-related diseases.

D(+)-Raffinose pentahydrate is an orally active inhibitor of LecA (K_d = 32 μM) and GtfC. D(+)-Raffinose pentahydrate reduces cyclic diguanylate (c-di-GMP) by increased activity of a c-di-GMP specific phosphodiesterase. D(+)-Raffinose pentahydrate interferes with GTF function. D(+)-Raffinose pentahydrate decreases IL-4 and IL-5 mRNA. D(+)-Raffinose pentahydrate exhibits biofilm-inhibitory activity against Pseudomonas aeruginosa and Streptococcus mutans and inhibits allergic airway eosinophilia.

Suplatast Tosilate (IPD 1151T) is an orally active Th2 cytokine inhibitor which can inhibit both IL-4 and IL-5 production from Th2 cells and suppress IgE synthesis. Suplatast Tosilate is an anti-allergic agent. Suplatast Tosilate has antiasthmatic, anti-inflammatory and antifibrotic activity.

(±)-Praeruptorin A, a coumarin compound, is the main bioactive component in Peucedani Radix. As a calcium channel blocker, (±)-Praeruptorin A exhibits great antihypertensive effects. In addition, (±)-Praeruptorin A also has the effects of relaxing vascular smooth muscle, inhibiting airway inflammation and airway hyperresponsiveness. (±)-Praeruptorin A can be used for the research of allergic asthma, hypertension and other diseases.

Luteolin-4'-O-glucoside is an IL-5 inhibitor with an IC₅₀ of 3.7 μM. Luteolin-4'-O-glucoside resists hyperuricemia and acute gouty arthritis activity. Luteolin-4'-O-glucoside shows anticancer activity.

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.

Lyn peptide inhibitor (YGYRLRRKWEEKIPNP-NH₂) is a potent, cell-permeable Lyn kinase inhibitor that inhibits Lyn-coupled signaling pathways associated with the IL-5 receptor while preserving the integrity of other signals. Lyn peptide inhibitor blocks the activation of Lyn and inhibits the binding of Lyn tyrosine kinase to the βc subunit of the IL-3/GM-CSF/IL-5 receptor. Lyn peptide inhibitor can be used in the research of eosinophilic diseases such as asthma and allergy.

Revbekitug is a humanized IgG1κ antibody targeting IL-5. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).

NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC₅₀ of 182 nM.

AN-2898 is a selective PDE4 inhibitor with IC₅₀ of 0.027 μM over other phosphodiesterase enzymes, such as PDE1A, PDE2A and PDE3A. AN-2898 also potently inhibits PDE4 subtypes (PDE4B1, PDE4A1A and PDE4D2). AN-2898 significantly inhibits the production of TNF-α, IL-2, IFN-γ, IL-5 and IL-10. AN-2898 can be used for mild to moderate atopic dermatitis (AD) and psoriasis research.