T-lymphocyte

PD-1/PD-L1-IN-10 is an orally available PD-1/PD-L1 inhibitor (IC50 value of 2.7 nM) that shows anti-tumor activity.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Inosine pranobex (Delimmun) has a number of immunomodulatory effects, including inducing T-lymphocyte differentiation, augmenting macrophage and NK cell functions, and stimulating IL-2 production. Through these effects and others, isoprinosine shows antiviral activity and has applications against subacute sclerosing panencephalitis. It also restores depressed immune responses in Y patients after irradiation and reduces the incidence of infection in leukemia patients undergoing chemotherapy. It is most commonly used to treat the rare measles complication subacute sclerosing panencephalitis in conjunction with intrathecal interferon therapy.

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

Aspartyl-alanyl-diketopiperazine acetate (DA-DKP) (DA-DKP) can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.

Forodesine (BCX-1777) is an orally active and potent purine nucleoside phosphorylase (PNP) inhibitor, a new purine nucleoside analog, inhibitor of human lymphocyte proliferation, induces apoptosis in leukemic cells by increasing dGTP levels, and may be useful in the study of cutaneous T-cell lymphomas.

TC-S 7003 (Lck Inhibitor) is an orally active, selective and potent lymphocyte kinase (Lck) inhibitor with anti-inflammatory activity, inhibition of Lck, Lyn, Src, and Syk kinases, and inhibition of T-cell proliferation, and may be useful in the study of arthritis.

NKH477 (Colforsin dapropate hydrochloride) is a derivative of forskolin with antidepressant activity. It inhibits ACh-induced Ca2+ mobilization by acting on ionomycin-sensitive storage sites. NKH477 is an adenylyl cyclase activator with bronchodilatory effects, inhibiting the production of CTL, T-cell proliferation in mixed lymphocyte reactions (MLR), as well as IL-2 production and mitogen responses.

PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting ly

PF-07265028 is an HPK1 inhibitor with an IC50 of 17 nM. Pharmacokinetic studies in mice and monkeys indicate that PF-07265028 exhibits moderate clearance, terminal half-life, volume of distribution, and oral bioavailability. It targets, binds, and inhibits Hpk1 activity, blocking Hpk1-mediated signaling pathways to prevent immune suppression mediated by Hpk1, including the inhibition of T-cell receptor (TCR) signaling, effector T-cell suppression, aberrant cytokine expression, and the elimination of the immunosuppressive tumor microenvironment (TME). This action can activate a cytotoxic T lymphocyte (CTL)-mediated immune response against tumor cells. Hpk1 is primarily expressed in hematopoietic cells and acts as a negative regulator of TCR signaling and T and B cell activation.

Tubulin polymerization/V-ATPase-IN-1 (compound F10) is an inhibitor of tubulin polymerization and V-ATPase. It exhibits potent antiproliferative activity against four types of human cancer cells by inhibiting both tubulin and V-ATPase. The compound also induces apoptosis and immunogenic cell death while suppressing tumor growth in the RM-1 allograft model with enhanced T lymphocyte infiltration.

BC12 exhibits unusually potent immunomodulatory actions on T lymphocyte function, including inhibition of T cell proliferation and IL-2 cytokine production.

DMI-9523 is nuclear factor NF-κB activation inhibitor. Antigen-stimulated human T lymphocytes produce significantly lower quantities of interferon-gamma and tumor necrosis factor-alpha after stimulation in vitro in the presence of DA-DKP. DA-DKP can modul

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.

Tetranactin is a macrotetrolide and a monovalent cation ionophore that has been found in S. aureus and has antibacterial, insecticidal, and mitogenic activities. It exhibits an equilibrium permeability ratio 1,000-fold greater for lithium than sodium or cesium ions accross bilayer membranes at low voltages. Tetranactin inhibits the growth of Gram-positive bacteria and C. miyabeanus and R. solani fungi when used at concentrations less than 0.9 μg/ml. Tetranactin (0.5-1.5 μg per insect) dose-dependently increases the mortality of adult C. chinensis weevils up to 100% and has mitogenic activity against T. telarius when sprayed onto plants with an LC50 value of 9.2 μg/ml. It reduces IL-1β- and cAMP-induced secretion of phospholipase A2 (PLA2) from rat mesangial cells (IC50s = 43 and 33 nM, respectively). Tetranactin (50 ng/ml) suppresses the proliferation of human T lymphocytes induced by allogeneic cells and IL-2 and supresses the generation of cytotoxic T lymphocytes in mixed lymphocyte cultures. In vivo, tetranactin (10 mg/animal per day) completely inhibits the formation of experimental autoimmune uveoretinitis (EAU) in rats.

Azido-FTY720 (azido-Fingolimod) is an analogue of FTY720 featuring an azido group suitable for click chemistry reactions. FTY720 is an orally available S1P analogue and S1P1R modulator capable of crossing the blood-brain barrier (BBB), reducing neuroinflammation, and is indicated for multiple sclerosis (MS).

NS2 (114-121), Influenza, is a fragment derived from the nonstructural protein 2 (NS2) of the influenza virus, serving as an epitope for influenza research and useful for studying CD8+ cytotoxic T lymphocyte (CTL) responses in antiviral immunity.

Lifitegrast sodium (SAR-1118-023 sodium) is a small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), which reduces inflammation of the ocular surface, and may be used in the study of dry eye.

Enhanced Green Fluorescent Protein (200-208) (EGFP (200-208)) is a peptide that strongly binds to H2-K, a restricted cytotoxic T lymphocyte (CTL) epitope.

CXCR2 antagonist 3 (compound 11h) is a highly effective inhibitor of CXC chemokine receptor 2 (CXCR2), displaying double-digit nanomolar potencies in inhibiting neutrophil infiltration into the air pouch. Additionally, it reduces neutrophil and MDSC infiltration while enhancing CD3+ T lymphocyte infiltration into Pan02 tumor tissues [1].

RORγt agonist 3 is a potent agonist of RORγt that induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines, and enhances lymphocyte cytotoxicity. Moreover, [it] blocks the production of regulatory T cells and suppresses the immune response.

RORγt agonist 2 is a potent agonist of RORγt that induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines, and enhances lymphocyte cytotoxicity. It exhibits an inhibitory effect on the production of regulatory T cells and can suppress immune responses.