killer,cells

Loxoribine (RWJ 21757) is a guanosine analog. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist. It has anti-viral and anti-tumor activities.Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities.

Amivantamab (JNJ-61186372) is a humanized antibody that recognizes epidermal growth factor receptor (EGFR) and MET proto-oncogene (MET), with anticancer and anti-tumor activities, preventing ligand binding to EGFR and MET and receptor dimerization that inhibits downstream signal transduction. Amivantamab can induce Fc-dependent endocytosis of macrophages and antibody-dependent cytotoxicity of natural killer cells, and can be used to study metastatic non-small cell lung cancer.

CP-31398 stabilizes the active conformation of p53 in cancer cells with either mutated or wild-type p53, enhancing its activity. Additionally, CP-31398 upregulates target genes of p53 such as p21WAF1 Cip1 and KILLER DR5. This compound possesses tumor-suppressive properties.

Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ubiquitin ligase Cbl, demonstrating an IC50 of 15 nM. Cbl-b refers to Casitas B-lineage Lymphoma proto-oncogene-b, which can inhibit the activation of T cells, natural killer (NK) cells, and B cells. Cbl-b-IN-15 can activate T cell function with an EC50 of 0.41 μM.

Adenanthin, a natural inhibitor of thiol-dependent antioxidant enzymes, impairs the effector functions of human natural killer cells.

C8 Galactosylceramide is a synthetic C8 short-chain derivative of known membrane microdomain-forming sphingolipids. It increases the amount delivered and toxicity of doxorubicin in cancerous but not non-cancerous cells when incorporated into the nanoliposomal membrane of nanoliposomal-doxorubicin. C8 Galactosylceramide induces proliferation and cytokine production by splenocytes in vitro at concentrations ranging from 100-1,000 ng ml but has no effect on natural killer T cell production in vivo. It also activates NF-κB production in C6 glioma cells when used at a concentration of 10 μM.

C12 Galactosylceramide is a bioactive sphingolipid. It inhibits IL-4 production by 53.84% in EL4 T cells when used at a concentration of 10 μM. C12 Galactosylceramide reduces the growth of human papillomavirus type 16-associated tumors in mice and reduces tumor recurrence following surgical removal or chemotherapy. It also reduces natural killer T cell activity, delays the onset of proteinuria, and improves survival in a mouse model of systemic lupus.

H-Leu-Leu-OMe HBr (L-Leucyl-L-Leucine methyl ester HBr) is a dipeptide condensation product of L-Leucine methyl ester, a peptide that is toxic to natural killer T-cells and possesses immunosuppressive activity that abrogates all natural killer (NK) cell functions in mixed lymphocyte populations.

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

NZ28, also known as NSC134754, is potent HSF1 inhibitor, which induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA B on human tumor cells. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis.

NLG802 is an orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, the indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs).

ANA773 is a Toll-like Receptor 7 (TLR7) agonist prodrug with potential immunostimulating activity. Upon oral administration, ANA773 is metabolized into its active form that binds to and activates TLR7, thereby stimulating dendritic cells (DCs) and enhancing natural killer cell (NK) cytotoxicity. This activation results in the production of proinflammatory cytokines, including interferon alpha, and enhanced antibody-dependent cellular cytotoxicity (ADCC). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.

αGalCer-RBD, a conjugate of the potent invariant natural killer T cell (iNKT) agonist α-Galactosylceramide (αGalCer) and the receptor-binding domain (RBD), serves as a self-adjuvanting lipoprotein that exhibits strong potential as a COVID-19 vaccine candidate. This compound effectively induces immunity against SARS-CoV-2 and its variants of concern by promoting the development of RBD-specific, cytokine-producing T cells.

Mezagitamab (TAK-079) is a fully humanized IgG1λ monoclonal antibody against CD38 with high affinity for CD38-expressing cells (including plasma mother cells, plasma cells, and natural killer cells), which depletes CD38-expressing tumor cells through antibody- and complement-dependent cytotoxicity Mezagitamab may be used in the study of recurrent/refractory multiple myeloma (RRMM), which is the most common form of cancer. multiple myeloma (RRMM) and primary thrombocytopenic purpura (ITP).

Urelumab(BMS-66513) is a humanized IgG4 monoclonal antibody, often used as a CD137 agonist.Urelumab has potential antitumor activity, potentiating tumor cell killing by T-cells and natural killer cells, and enhancing the cytotoxicity of Rituximab.Urelumab has been used in the study of solid tumor-related diseases such as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL). Urelumab can be used to study diseases associated with solid tumors such as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL).

Lirilumab (IPH2102) is an antibody against the lethal immunoglobulin-like receptor antibody KIR2D with antitumor activity that enhances the anti-HPV + cervical cancer activity of natural killer cells through VAV1-dependent NF-κB deinhibition. It can be used to study leukemia, head and neck squamous cell carcinoma (SCCHN).

Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor that irreversibly inhibits H+/K+-ATPase in rabbit parietal cells with a dose-dependent IC50 of 6 μM. It is used in gastric ulcer research and acts as a potent inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK) [1] [2].

Peptide A5K acetate (INF7-A5K-TAT acetate) is an amphiphilic peptide derived from the HA2-TAT fusion scaffold, designed to facilitate macromolecular transport in genome editing. Peptide A5K acetate non-covalently binds to CRISPR RNP (ribonucleoprotein complex) and delivers it into cells such as primary human T cells, B cells, and NK cells, enabling low-toxicity, multi-target, highly efficient, and precise genome editing.

Lorukafusp alfa (14.18 mAb; hu14.18-IL2) is an immunocytokine composed of a humanized 14.18 anti-GD2 monoclonal antibody (mAb) linked to interleukin-2 (IL2). It exerts anti-tumor effects [1] by inducing antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity, targeting GD2-expressing tumor cells, and stimulating NK and T cells via IL2 receptors.

Euphoscopin C, a diterpenoid isolated from Euphorbia helioscopia, significantly enhances the cytotoxic activity of natural killer (NK) cells against H1299-luci and A549-luci cells [1].

Euphoheliosnoid A (Compound 24), a diterpenoid, significantly enhances natural killer (NK) cell-mediated cytotoxicity against H1299-luci cells and A549-luci cells at a concentration of 2.5 μM [1].

Deacetylasperulosidic Acid is a natural compound of Morinda citrifolia fruit. It has antioxidant activity by increasing superoxide dismutase activity. It also prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells.

MTX-3937, a Siglec-9 inhibitor with a dissociation constant (Kd) of 3.15 μM, enhances the function and homeostasis of natural killer (NK) cells. Furthermore, MTX-3937 significantly improves the anti-hepatocellular carcinoma efficacy of NK cell-mediated antitumor activity in vivo.

GCS-12, a Th1 2-balanced sulfonamide glycolipid, enhances its interaction with CD1d. It acts as an agonist for Natural Killer T cells (NKT cells), inducing the secretion of cytokines IFN-γ and IL-4. In mice, it has demonstrated immunoregulatory and antitumor activities.