LAG-3

PF 06465469 is a potent the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase) inhibitor. It also inhibits BTK.

Ieramilimab (LAG525; IMP701) is a humanized IgG4 monoclonal antibody designed to target and bind to lymphocyte-activation gene 3 (LAG-3). This interaction effectively inhibits the binding of LAG-3 to major histocompatibility complex class II (MHC-II) molecules, which is critical in modulating immune response. Ieramilimab is utilized extensively in research focused on immune checkpoint regulation and potential therapeutic interventions for various immunological disorders.

Tebotelimab (MGD-013) is a humanized IgG4κ bispecific antibody designed for dual affinity re-targeting (DART) of PD-1 and LAG-3. This therapeutic agent demonstrates high affinity binding to cell-surface expressed PD-1 and LAG-3, with half-maximal effective concentrations (EC50s) of 1.65 nM and 0.41 nM in NS0 cells, respectively. By effectively blocking the interactions between PD-1/PD-L1, PD-1/PD-L2, and LAG-3/HLA (MHC-II), as well as inhibiting PD-1 signaling pathways, Tebotelimab plays a crucial role in restoring the function of exhausted T-cells. This restoration is pivotal in enhancing anti-tumor immunity, making Tebotelimab a significant tool in cancer immunotherapy research.

Bavunalimab is a bispecific monoclonal antibody targeting CTLA-4 and LAG-3, designed for the dual inhibition of these immune checkpoint inhibitors. This humanized antibody promotes T-cell activation, demonstrated in NSG mouse models, making it a valuable tool for investigating immune responses in oncology research. Bavunalimab is specifically developed for studies focusing on the modulation of immune checkpoints in cancer therapy.

Encelimab is a monoclonal antibody targeting LAG-3 (Lymphocyte-activation gene 3). By inhibiting the interaction between LAG-3 and MHC class II molecules, Encelimab promotes T-cell activation and enhances immune responses. Studies have demonstrated that Encelimab, both as a monotherapy and in conjunction with an anti-PD-1 antibody, effectively reduces tumor volume in a lymphoma mouse model using A20 cell xenografts. This antibody is pivotal for research focused on immunotherapy and cancer immunology, particularly in understanding and manipulating T-cell responses in oncological models.

Favezelimab (MK-4280) is a humanized monoclonal antibody targeting LAG-3, designed to inhibit the binding of LAG-3 to MHC class II molecules. This interaction blockade enhances T-cell function and may potentiate an anti-tumor immune response. Favezelimab is primarily investigated for its therapeutic potential in colorectal cancer research, particularly in combination with the PD-L1 inhibitor Pembrolizumab, to synergistically enhance immune-mediated tumor suppression.

Fianlimab (REGN3767) is a human monoclonal antibody designed to specifically bind to the lymphocyte-activation gene 3 (LAG-3) immune checkpoint receptor expressed on T cells. This interaction inhibits the LAG-3 pathway, thereby enhancing T cell function and exhibiting potent anti-tumor activity. Fianlimab is utilized in oncological research to investigate immune checkpoint blockade as a strategy for cancer immunotherapy.

Tuparstobart (Incagn-02385) is an IgG1κ monoclonal antibody designed to specifically target LAG-3, an immune checkpoint receptor. LAG-3 is predominantly expressed on activated T cells, NK cells, B cells, and plasmacytoid dendritic cells. This antibody is engineered to bind to LAG-3, thereby modulating immune responses, which may be critical in the research of immune regulation and potential therapeutic applications in immune-related disorders.

Relatlimab (BMS-986016) is a human monoclonal antibody targeting LAG-3, developed through the immunization of transgenic mice engineered to express human immunoglobulin miniloci, using recombinant LAG-3 protein. This antibody effectively inhibits the interaction between LAG-3 and MHC II with an IC50 of 0.67 nM, and between LAG-3 and FGL1 with an IC50 of 0.019 nM. It is primarily utilized in cancer research, providing a valuable tool for investigating the role of LAG-3 in tumor immune evasion and potential therapeutic interventions.

Miptenalimab (BI-754111) is a monoclonal antibody targeting human LAG-3 with a dissociation constant (K_D) of 88.6 nM. This antibody effectively inhibits the interaction between LAG-3 and its physiological ligand MHC class II, highlighting its potential utility in modulating immune responses in oncological and immunological research.

Negalstobart is a human IgG4 κ monoclonal antibody targeting LAG-3. For control experiments, it is recommended to use Human IgG4 (S228P) kappa as an isotype control.

RBN013209 is an orally active, small molecule inhibitor of CD38, exhibiting potent inhibitory activity with an IC₅₀ ranging from 0.01 to 0.1 μM against human CD38. It effectively blocks the enzymatic conversion of extracellular NAD⁺ to ADPR and cADPR in both tumor cells and peripheral blood mononuclear cells (PBMCs), thereby modulating the tumor microenvironment. Beyond its direct antitumor potential, RBN013209 also enhances the efficacy of immunotherapies. It preserves the naïve and central memory phenotypes of CAR-T cells, while reducing the expression of activation markers and exhaustion-associated inhibitory receptors. These properties position RBN013209 as a promising agent for both tumor research and the development of combination strategies to improve CAR-T cell persistence and function.

DAPK1 ligand-1 is a PROTAC target protein ligand designed for the synthesis of PROTACs, including the DAPK1 Degrader-1. This compound facilitates the targeted degradation of LAG-3, demonstrating significant neuroprotective activity. Its application in research underscores its utility in studying the modulation of immune checkpoints and neuroprotection mechanisms in various biological contexts.

A2AR-antagonist-1 is a selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 29 nM. This compound demonstrates significant anti-tumor activity and maintains metabolic stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, A2AR-antagonist-1 activates T cells by inhibiting immunosuppressive molecules such as LAG-3 and TIM-3, while promoting the expression of effector molecules including GZMB, IFNG, and IL-2, making it a valuable tool in cancer immunotherapy research.

LAG-3 degrader 1 is a PROTAC target protein ligand designed for the synthesis of PROTACs targeting LAG-3. This compound facilitates the targeted degradation of LAG-3, demonstrating significant anti-tumor activity. It serves as a valuable tool in cancer research, allowing for the exploration of LAG-3 modulation in therapeutic applications.

LAG-3 biner 1 is a small molecule ligand that specifically targets the immune checkpoint lymphocyte activation gene 3 (LAG-3), exhibiting a Kd of 1.23 μM. This compound plays a significant role in modulating immune responses and is valuable for research applications focused on cancer diagnostics and the exploration of immune regulation involving LAG-3.

SA-15-P is a potent inhibitor of the LAG-3/MHCII and LAG-3/FGL1 protein-protein interactions, with IC50 values of 4.21 μM and 6.52 μM, respectively. By disrupting these interactions, SA-15-P serves as a valuable tool in immunotherapy research, providing insights into immune regulation and the potential enhancement of anti-tumor responses. Its application facilitates the exploration of therapeutic strategies targeting LAG-3 in various disease contexts.

LAG-3-IN-2 is a selective inhibitor of LAG-3 (Lymphocyte Activation Gene 3), a key immune checkpoint involved in the regulation of T cell responses. By blocking LAG-3, this compound enhances T cell activation and proliferation, making it a valuable tool in immunological research. It is particularly relevant in studies focused on cancer immunotherapy and autoimmune diseases, where modulation of immune responses is critical.

Z3071585108 is a small molecule inhibitor of the LAG-3 D1 domain, exhibiting Kd values of 59.2 μM and 56.1 μM through MST-TRIC channel and spectral shift detection, respectively. This compound partially inhibits the interaction between LAG-3 and MHC class II molecules, with an EC₅₀ value of 42.9 μM. Z3071585108 is valuable for research on small molecule immunotherapies targeting the LAG-3 pathway, contributing to the understanding of immune modulation in various diseases.