TNF Receptor Agonist

Dordaviprone (TIC10) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. Dordaviprone can cross the blood-brain barrier.

Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC₅₀=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC₅₀=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.

Conatumumab (AMG 655) is a human monoclonal agonist antibody against human death receptor 5 (DR5, TRAILR2) (K_d: 1 nM for the long form of DR5, 0.8 nM for the short form of DR5). Conatumumab induces apoptosis via caspase activation. Conatumumab can be used in the research of cancers. .

Selicrelumab is an agonist CD40 antibody, induces changes in the tumor microenvironment. Selicrelumab can be used for the research of pancreatic cance and neoadjuvant study.

MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities K_d ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)).

Sotigalimab, a CD40 agonistic monoclonal antibody. Sotigalimab binds CD40 with high affinity and activates antigen-presenting cells, thereby stimulating cancer-specific T cell responses. Sotigalimab is mainly used in the study of metastatic pancreatic cancer and metastatic melanoma.

Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC₅₀=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.

JNU-0921 is a potent and orally active CD137 agonist. JNU-0921 increases the mRNA expression of IFN-γ and GZMB. JNU-0921 induces luciferase activity with an EC₅₀ value of 64.07 nM.JNU-0921 enhances effector and memory function of cytotoxic CD8⁺ T cells (CTLs) and alleviates their exhaustion. JNU-0921 also skews polarization of helper T cells toward T helper 1 type and enhances their activity to boost CTL function. JNU-0921 shows anticancer activity.

Ragifilimab (INCAGN-1876) is an agonist monoclonal antibody targeting the glucocorticoid-induced TNFR-related protein (GITR). Ragifilimab binds to and activates GITR on T cells, which stimulates the immune system to enhance its anti-tumor activity. Ragifilimab can be used for advanced or metastatic solid tumors research.

TBPH is a brominated flame retardant. TBPH enhances hepatic steatosis, inflammation, and fibrosis in mice with nonalcoholic steatohepatitis (NASH). TBPH induces dysregulation of phospholipid metabolism, reducing cardiolipin (CL) and phosphatidylserine (PS) levels. TBPH leads to impaired endoplasmic reticulum-mitochondria (ER-Mito) contacts, subsequently causing mitochondrial dysfunction. TBPH induces lung injury through an inflammatory response mediated by mitochondria-derived ds-DNA. TBPH can be used to study the role of MFN2-mediated ER-mitochondria contacts in lipid metabolism homeostasis.

Anti-Mouse GITR Antibody (DTA-1) is a rat derived IgG2b monoclonal agonist antibody targeting mouse GITR. Anti-Mouse GITR Antibody (DTA-1) can activate T cells and B cells to enhance immune response. Anti-Mouse GITR Antibody (DTA-1) selectively enhances Th2 cell effector function through GITR signaling. Anti-Mouse GITR Antibody (DTA-1) may exacerbate allergic reactions. Anti-Mouse GITR Antibody (DTA-1) can be used for researches on cancer and allergic conditions such as colon cancer and allergic asthma. The recommed isotype control of Anti-Mouse GITR Antibody (DTA-1) is Rat IgG2b kappa, Isotype Control (HY-P990682).

Aplitabart (IGM-8444) is a pentameric IgM death receptor 5 (DR5) agonist antibody with a K_D of 85 nM and an apparent affinity of 11 pM. Aplitabart induces DR5 multimerization, thereby triggering cancer cell apoptosis via the extrinsic apoptotic pathway apoptosis. Aplitabart is applicable to cancer-related research such as colorectal cancer and gastric cancer.

MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer.

Benufutamab (GEN1029) is a death receptor 5 (DR5)-specific agonistic antibody. Benufutamab is a mixture of 2 noncompeting DR5-specific IgG1 antibodies, each with an E430G mutation in the Fc domain. Benufutamab has antitumor effects.

STING agonist-45 is a selective STING agonist (EC₅₀ = 0.28 μM). STING agonist-45 activates the innate immune response through the cGAS-STING pathway, upregulating key markers such as p-TBK1 and IRF3. STING agonist-45 exhibits robust STING activation in human peripheral blood mononuclear cells (PBMCs), inducing the production of type I interferons (such as IFN-β) and downstream cytokines (such as TNF-α and IL-6). STING agonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8⁺ T cell infiltration in mouse models. STING agonist-45 is promising for the study of STING-related diseases.

MK-4166 is a humanized IgG1 agonist monoclonal antibody targeting GITR. MK-4166 enhances the proliferation of both naïve and tumor-infiltrating T lymphocytes.

BMS-986156 is a fully humanized IgG1 agonist monoclonal antibody agonist corticosteroid-induced tumor necrosis factor receptor-related protein (GITR). BMS-986156 binds to GITR and promotes activation of T effector cells and inactivates T regulatory cells. BMS-986156 is indicated for use in advanced solid tumor studies.

2141-V11 is an anti-CD40 agonist antibody with enhanced binding to FcγRIIB. 2141-V11 results in effective tumor-specific T-cell responses in vivo. 2141-V11 can be used for the study of BCG-unresponsive non-muscle invasive bladder cancer.

MG-C-30 is an orally active agonist for CD27 with an EC₅₀ of 0.84 μM. MG-C-30 activates NK cells and T cell co-stimulatory signals, and enhances immune response. MG-C-30 exhibits antitumor efficacy in mouse EG7-OVA model.

PTX-35 is a costimulatory agonist antibody targeting TNFRSF25 as well as an immune activator that selectively regulates activated CD8⁺ T cells. PTX-35 enhances the expansion, survival and effector functions of T cells, while reducing the inhibitory activity of regulatory T cells and impairing their stability. PTX-35 exhibits anti-tumor activity, effectively delaying tumor progression and prolonging survival. PTX-35 has a synergistic effect with anti-OX40 agonist antibodies. PTX-35 can be widely used in research on related diseases such as colon cancer and melanoma.