jurkat

Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

Andrograpanin (19-HYDROXY-8(17),13-LABDADIEN-16,15-OLIDE) is a bioactive compound from Andrographis paniculata. Andrograpanin has anti-inflammatory and anti-infectious properties.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Necrostatin-5 (Nec-5) is a selective RIP1 kinase inhibitor and cell necrosis inhibitor that prevents the death of Fadd-deficient Jurkat cells treated with TNF-α, with an EC50 of 240 nM.

2-Nitrobenzoic acid (o-Nitrobenzoic acid) is a antiproliferation agent. 2-Nitrobenzoic acid shows IC50 of 8.3 μM to jurkat cell line expressing T type calcium channel alpha 1H or its splice variant delta 25.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Squalene (AddaVax) is a natural organic compound originally obtained for commercial purposes primarily from shark liver oil, though there are botanical sources as well, including rice bran, wheat germ, and olives. All higher organisms produce squalene, including humans. Squalene is an intermediate product in the synthesis of cholesterol and shows several pharmacological properties such as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity.

Myricetin (Cannabiscetin) is a natural flavonoid and MEK1 inhibitor. Myricetin has hypoglycemic, antioxidant, hepatoprotective, anti-tumor and anti-inflammatory activities.

Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50:10 39 nM).

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

Tulipalin A (α-methylene-γ-butyrolactone) (2-Methylenebutyrolactone) which has some phytotoxicity is a natural compound extracted from Tulipa gesneriana.

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

QNZ (EVP4593) (EVP4593) is an effective inhibitor of NF-κB activation and TNF-α production. The IC50 of QNZ for NF-κB and TNF-α is11 nM and 7 nM, respectively.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Neoandrographolide (Neoandrographiside) has potent hypolipidemic effect and protects the cardiovascular without significant liver damage.Neoandrographolide has anti-inflammatory effect, might result from inhibition of iNOS and COX-2 expression through inhibiting p38 MAPKs activation.Neoandrographolide as chemosensitizer in S-Jurkat and X chromosome-linked inhibitor of apoptosis protein (XIAP)-overexpressing Jurkat cells, a model for chemoresistance.

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

TJ191 is a selective anti-cancer agent, targeting low TβRIII-expressing malignant T-cell leukemia lymphoma cells.

SP-100030 is a dual inhibitor of NF-κB and activator protein-1 (AP-1), demonstrating potent inhibition with IC50 values of 50 nM for both. It effectively reduces the production of IL-2, IL-8, and TNF-alpha in Jurkat and other T cell lines. Additionally, SP-100030 has been shown to decrease the severity of murine collagen-induced arthritis (CIA).

Milategrast is a chemical compound that functions as a potent cell adhesion inhibitor and cell infiltration inhibitor. In vitro studies have demonstrated its ability to effectively inhibit the adhesion of Jurkat cells to human fibronectin, with an IC50 value of less than 5 μM.

Irreversible MALT1 inhibitor. Suppresses T cell activation-induced cleavage of Bcl-10 in a dose-dependent manor. Reduces Jurkat cell adhesion to fibronectin. Cell permeable.

LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 25 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 334 and 4,214 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 protein-protein interaction. J. Med. Chem. 62(15), 7250-7263 (2019).

PROTAC CDK4 6 degrader 1 (Compound 7f) is a dual degrader of CDK4 and CDK6, with DC50 values of 10.5 nM and 2.5 nM, respectively. This compound effectively inhibits proliferation in Jurkat cells (IC50 of 0.18 μM), induces cell cycle arrest during the G1 phase, and triggers cell apoptosis (apoptosis).

EPI-X4, an endogenous peptide fragment of human serum albumin (amino acids 408-423), serves as an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4). It effectively prevents calcium mobilization and receptor internalization triggered by chemokine (C-X-C motif) ligand 12 (CXCL12) in HEK293 cells with CXCR4 expression, at concentrations between 0.8 and 1,000 µM. Moreover, EPI-X4 hampers the CXCL12-driven migration of both Jurkat T cells and human CD34+ hematopoietic stem cells. In an acute allergic airway hypereosinophilia mouse model, EPI-X4 intrinsically decreases Cxcr4-dependent inflammatory cell infiltration in airways at a dose of 16 µmol/kg. Additionally, increased urinary EPI-X4 levels, inversely related to glomerular filtration rate (GFR), are observed in chronic kidney disease patients, indicating its potential biomarker role.