IL-2 Inhibitor

Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.

Daclizumab (Ro 24-7375) is a humanized, monoclonal antibody that blocks CD25 (α-subunit of the high-affinity interleukin-2 receptor (IL-2R-HA)). Daclizumab inhibits effector T cell activation, regulatory T cell (Treg) expansion and survival, and activation-induced T-cell apoptosis. Daclizumab increases IL-2 bioavailability to bind to the intermediate-affinity IL-2R (IL-2R-IA), driving the expansion of anti-inflammatory CD56bright natural killer (NK) cells. Daclizumab can be used for multiple sclerosis and cancer research.

Imneskibart (AU-007) is a human monoclonal antibody that binds to the CD25-binding epitope of interleukin-2 (IL-2), blocking the binding of IL-2 to the trimeric IL-2 receptor while retaining the ability to bind to the dimeric IL-2 receptor. Imneskibart expands effector T cell and NK cell populations, reduces regulatory T cells, increases the effector T cell/regulatory T cell ratio, and alleviates vascular leakage. Imneskibart can be used in research related to melanoma and non-small cell lung cancer. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).

BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1). BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.

IBI-363 is a PD-1/IL-2 bispecific antibody with functions of blocking the PD-1/PD-L1 pathway and activating the IL-2 pathway. The IL-2 arm of IBI-363 retains affinity for IL-2Rα but attenuates binding ability to IL-2Rβ and IL-2Rγ to reduce toxicity. The PD-1 binding arm of IBI-363 enables PD-1 blockade and selective delivery of IL-2. IBI-363 can be used in cancer research, such as non-small cell lung cancer.

Anti-Mouse IL-2 Antibody (JES6-1A12) is an anti-mouse IL-2 IgG1 monoclonal antibody. Anti-Mouse IL-2 Antibody (JES6-1A12) can inhibit Treg amplification and enhance Th1 response. Anti-Mouse IL-2 Antibody (JES6-1A12) can form a complex with IL-2 for experimentation. Anti-Mouse IL-2 Antibody (JES6-1A12) can be used for research on infection conditions such as malaria.

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.

PQA-18 is a unique PAK2 inhibitor (IC₅₀: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice.

Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection).

Deacetylasperulosidic Acid is an orally active antioxidant. Deacetylasperulosidic Acid exerts a definite in vivo antioxidant effect and alleviates oxidative stress injury by enhancing SOD activity. In atopic dermatitis models, Deacetylasperulosidic Acid corrects Th2-skewed immune imbalance and reduces allergy-related factors; in immunosuppression models, it activates cellular immunity, enhances NK cell activity and IL-2 production. Deacetylasperulosidic Acid can be used in the research of atopic dermatitis.

Vopikitug is an IgG1-kappa, anti-IL2RA (interleukin 2 receptor alpha subunit, IL-2RA, TAC, p55, CD25) homo sapiens monoclonal antibody. Vopikitug shows antineoplastic activity.

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.

CMD178 TFA is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits T_reg cell development.

Sec61-IN-3 is a Sec61 inhibitor. Sec61-IN-3 shows a significant inhibitory effect on PD-1 related reporter gene cell models (PD1tsGluc) (IC₅₀ = 42 nM), and also has certain inhibitory activity on Her3 (IC₅₀ = 99 nM), IL2 (IC₅₀ = 144 nM) related reporter pathways, but has a relatively weak inhibitory effect on the TNFα (IC₅₀ = 580 nM) pathway. Sec61-IN-3 can be used for cancer research.

Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

SP4206 is an IL-2/IL-2Rα interaction inhibitor. SP4206 binds with high affinity (K_d=70 nM) to IL-2 and blocks binding to its natural receptor IL-2Rα (K_d=10 nM).

Patiromer is an orally active, selective and non-absorbable intestinal potassium (K⁺) polymer binder that reversibly binds potassium ions in exchange for calcium (Ca²⁺). Patiromer can rapidly and continuously reduce serum potassium levels, maintain a normal blood potassium state, and reduce serum aldosterone levels. Patiromer also increases fecal potassium excretion. Patiromer is mainly used in the study of hyperkalemia associated with diseases such as chronic kidney disease, diabetes, and heart failure, and is particularly suitable for improving renin-angiotensin-aldosterone system inhibitor (RAASi) therapy.

GNE-6893 is an orally active, selective HPK1 inhibitor with a K_i < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers.

M351-0056 is an orally active VISTA agonist with a K_d value of 12.60 μM. M351-0056 inhibits the activation of the JAK2-STAT2 pathway, reduces the phosphorylation levels of JAK2 and STAT2, and regulates type I interferon (IFN-I) and non-canonical NF-κB pathways. M351-0056 decreases the levels of cytokines (IFN-γ, IL-17A, TNF-α, IL-2 and IL-1β). M351-0056 improves imiquimod (HY-B0180)-induced psoriasis-like skin inflammation, reduces autoantibody levels, kidney damage and immune cell expansion in mice susceptible to chronic graft-versus-host disease and lupus, and delays the progression of systemic lupus erythematosus. M351-0056 can be used in research related to psoriasis-like dermatitis and systemic lupus erythematosus.

Anti-Mouse IL-2 Antibody (S4B6-1) is an anti-mouse IL-2 IgG2a monoclonal antibody. Anti-Mouse IL-2 Antibody (S4B6-1) can reduce CD4⁺ T cells and increase Tregs. Anti-Mouse IL-2 Antibody (S4B6-1) can induce Th17 cell differentiation. Anti-Mouse IL-2 Antibody (S4B6-1) can be used for research on cancer such as melanoma. The recommend isotype control of Anti-Mouse IL-2 Antibody (S4B6-1): Rat IgG2a kappa, Isotype Control (HY-P990679).