pbmc cells

BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release).

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

Rifampicin (Rifamycin AMP) is a broad-spectrum antibiotic. Rifampicin has a strong antibacterial effect against Mycobacterium tuberculosis and is also effective against gram-positive and gram-negative bacteria and viruses.

Azithromycin (CP 62993) is a macrolide antibiotic that primarily targets the 50S subunit of bacterial ribosomes. Azithromycin is commonly used in studies of bacterial infections.

Vicriviroc maleate (SCH-417690 (maleate))(Sch-417690) is a piperazine-based CCR5 receptor antagonist with activity against human immunodeficiency virus. The IC50 value is 0.91 nM in clinical development for the treatment of HIV-1.

PD 404182 is a human dimethylarginine dimethylaminohydrolase 1 (DDAH1) inhibitor with anti-angiogenic and antiviral activities, and can be used to study cardiovascular diseases and viral infections.

Oleanonic acid (3-Ketooleanolic Acid) is relatively non-toxic, hepatoprotective, and exhibits antitumor and andantiviral properties.

AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC).

Emtricitabine is a nucleoside reverse transcriptase inhibitor with anti-human immunodeficiency virus (HIV) and hepatitis B virus activity, with an EC50 value of 0.01 µM in PBMC cells, and can be used to study HIV infection.

AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.

GNE-0946 is an effective and selective RORγ/RORc/NR1F3 antagonist (inverse agonist) with an EC50 of 4 nM in HEK-293 cells. It inhibits IL-17 production in human PBMC cells (IC50 = 17 nM) and can be used in autoimmune disease research.

LRRK2-IN-15 is an inhibitor of LRRK2. It exhibits an IC50 value of 5 nM in PBMC cells and 1.5 μM for BCRP. This compound is utilized in the research of Parkinson's disease.

4''-C18 EGCG is an effective inhibitor of α-amylase and α-glucosidase, with IC50 values of 3.74 and 0.81 μM, respectively. This compound suppresses carbohydrate-hydrolyzing enzymes, reduces oxidative stress and inflammation, and exhibits anti-diabetic activity. Moreover, 4''-C18 EGCG downregulates pro-inflammatory cytokines and demonstrates cytotoxicity at 50 μM against primary human peripheral blood mononuclear cells (PBMC), as well as non-cancerous cell lines 3T3-L1 and HEK 293.

VZMC013 is a potent chemical probe targeting the MOR-CCR5 heterodimer, effectively inhibiting HIV-1 entry exacerbated by opioid compounds. It exhibits nanomolar binding affinity to both MOR and CCR5, inhibits CCL5-activated calcium mobilization, and significantly enhances anti-HIV-1BaL activity compared to previously reported bivalent ligands. In TZM-bl cells co-expressing CCR5 and MOR, VZMC013 demonstrates greater inhibition of viral infection than in cells expressing only CCR5. Additionally, VZMC013 blocks HIV-1 entry into peripheral blood mononuclear cells (PBMC) in a concentration-dependent manner and more effectively inhibits opioid-accelerated HIV-1 entry in phytohemagglutinin-activated PBMC than in opioid-free environments.

1,2-Naphthoquinone inhibits urease in bacteria and plants, induces apoptosis in PBMC cells, and exhibits inhibitory activity against hiCE, hCE1, hAChE, and hBChE.

HPK1-IN-43 (compound 9f) is an HPK1 kinase inhibitor with an IC50 value of 0.32 nM. It inhibits the phosphorylation of the downstream protein SLP-76 in PBMC cells and enhances the secretion of interleukin 2 (IL-2) and interferon-γ (IFN-γ). HPK1-IN-43 is applicable to cancer research.

TLR7 agonist22 (Compound 11a) is a selective TLR7 agonist with an IC50 value of 25.86 μM. It inhibits the secretion of cell HBsAg and effectively activates TLR7, inducing the release of TLR7-regulated cytokines IL-12, TNF-α, and IFN-α in human PBMC cells. TLR7 agonist22 shows promise for developing novel immunomodulatory drugs in HBV research.

ODN 2216 sodium is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. It induces significant production of IFN-α and IFN-β. The compound stimulates IFN-α through pDC (plasmacytoid dendritic cells) and produces IL-12(p40) via DC (dendritic cells). ODN 2216 triggers peripheral blood mononuclear cells (PBMC) to produce IFN-γ indirectly, mediated by IFN-α/β. Additionally, ODN 2216 sodium can activate NK cells and enhance IFN-γ production in TCR-triggered CD4+ T cells.

BX 513 hydrochloride (VUF 2274 HCl) is a selective CCR1 antagonist (Ki=0.04 µM) that concentration-dependently inhibits CCL18-induced acidification in THP-1 monocytes and suppresses RANTES- and CCL18-induced chemotaxis in peripheral blood mononuclear cells (PBMCs).

JTE-607 is a cytokine production inhibitor. JTE-607 induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells.

Kaempferitrin (Lespenephryl) has antidepressant-like effect related to the serotonergic system, principally 5-HT1A. Kaempferitrin exerts cytotoxic and antitumor effects against HeLa cells. Kaempferitrin stimulates glucose-metabolizing enzymes, promotes glucose homeostasis. Kaempferitrin exerts immunostimulatory effects on immune responses mediated by splenocytes, macrophages, PBMC and NK cells. Kaempferitrin induces cytotoxic effects to include: cell cycle arrest in G1 phase and apoptosis via the intrinsic pathway in a caspase-dependent pathway.

High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID:27966810