t cell

Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.

Mast cell degranulating peptide (28-49) is a bee venom depolarizer that enhances cGMP levels in cerebellum tablets of mice.

Mast Cell Degranulating Peptide HR-2 acetate from giant hornet Vespa orientalis that has biological effects similar to mast cell degranulating peptide from bee venom.

Peptide from giant hornet Vespa orientalis that has biological effects similar to mast cell degranulating peptide from bee venom.

Cisplatin-resistant cells-IN-1 (Compound 8) exhibits high cytotoxicity against Cisplatin-resistant cells and effectively diminishes metabolic activity at low nanomolar concentrations, with an IC50 ranging from 0.14 to 1.79 μM in various resistant cell lines, including A549 A549-R, K562 K562-R, and MCF-7 MCF-7TamR [1].

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19 0.96 μM).

RO2959 Hydrochloride (RO2959 HCl) is a potent and selective inhibitor of CRAC channel(IC50: 402 nM). It is also a potent inhibitor of human IL-2.

Dazostinag disodium (TAK-676) is a synthetic novel interferon gene (STING) agonist that triggers STING signaling pathway activation and type I interferon activation. Dazostinag disodium (TAK-676) is also a highly effective immune system modulator with complete resolution and lasting memory of T cell immunity and the ability to promote lasting interferon-dependent anti-tumor immune responses.

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1 2 4 6 (IC50=36 47 510 1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

Cycloheximide (Naramycin A) is a natural product that reversibly inhibits translation elongation, is an antimitotic compound, and is an inhibitor of DNA and protein synthesis.

Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

SIRT6-IN-5(SIRT6 inhibitor 5) is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.

5-A-RU (5-Amino-6-(D-ribitylamino)uracil) is an early intermediate in riboflavin biosynthesis and is found in a variety of bacteria and yeast as well as plants. 5-A-RU is also a mucosal-associated invariant T (MAIT) cell activator that forms potent MAIT-activating antigens through non-enzymatic reactions with small molecules from other metabolic pathways.

(Rac)-SHIN2, a serine hydroxymethyltransferase (SHMT) inhibitor, enhances NOTCH1-driven in vivo survival of primary T-ALL in mice and is useful for studying T-cell acute lymphoblastic leukemia (T-ALL).

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

TP-16 is a novel potent and selective EP4 antagonist that blocks the function of IMCs and enhances cytotoxic T cell-mediated tumor elimination in vivo.

GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA).

Anisperimus (LF 15-0195) is an immunosuppressant that enhances activation-induced T-cell death by promoting caspase-8 and caspase-10 activation at the DISC level, and prevents CNS autoimmunity by promoting the development of Foxp3-expressing regulatory CD4 T cells.

KRM-III is an orally active T cell antigen receptor (TCR) inhibitor with anti-inflammatory activity that potently inhibits TCR and myristate acetate fosfomycin ionomycin-induced NFAT nuclear factor activation and T cell proliferation, with an IC50 of approximately 5 μM.

α-(difluoromethyl)-DL-Arginine (RMI 71897) is an enzyma-activated, irreversible inhibitor of arginine decarboxylase for E. coli (Ki = 800 μM), Pseudomonas aeruginosa, and Klebsiella pneumoniae. At 0.01 mM, it has been shown to prevent osmotic stress-induced increases in arginine decarboxylase activity and putrescine synthesis in oat leaf cells. When combined with a variety of polyamine analogues, α-(difluoromethyl)-DL-Arginine inhibited the growth of Trypanosoma Crui in mammalian host cells at a minimum concentration of 10 mM and prevented the growth of Trypanosoma Crui in T-cell receptor alpha-deficient mouse models.