pbmc cells

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).

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).

Indinavir sulfate (L735524 sulfate) is a HIV protease inhibitor.It inhibits the HIV-1 protease with an IC50 value of 0.41 nM and Ki value of 0.24 nM.

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

Mavorixafor (AMD-070) is an effective and selective antagonist of CXCR4, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells (IC50 = 1 nM) and PBMCs (IC50 = 9 nM).

ICeD-2, an inducer of cell death, effectively induces the killing of HIV-1 infected cells, a process reliant on HIV-1 protease activity. It significantly inhibits the hydrolysis of Gly-Pro-AMC by dipeptidyl peptidases DPP8 and DPP9, and robustly stabilizes DPP9 in peripheral blood mononuclear cells (PBMCs) [1].

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.

N6-(p-Methoxybenzyl)adenosine is an adenosine analog that shows in vitro antiproliferative activity in U87MG glioma cells and immunogenicity in isolated γδ T cells derived from stimulated peripheral blood mononuclear cells (PBMCs).

EIF2α Activator 1 (Compound 40) is a chemical compound that activates the phosphorylation of eukaryotic initiation factor 2 alpha (eIF2α), enhancing the expression of downstream proteins ATF and CHOP. It demonstrates antiproliferative effects against K562 and PBMC cells, with IC50 values of 4.00 and 19.3 μM, respectively [1].

Soyacerebroside II exhibits ionophoretic activity for Ca2+ ion. Soyacerebrosides I and II have modulating the cellular immune response effects, they show obvious inhibitory activity on IL-18 secretion in human peripheral blood mononuclear cells (PBMC).

ODN 2216 is a TLR9 (toll-like receptor 9) ligand or agonist that induces the production of large amounts of IFN-α and IFN-β. ODN 2216 can induce IFN-α using pDC (plasma cell-like DC) and IL-12 (p40) using DC (dendritic cells). ODN 2216 is capable of indirectly stimulating IFN-γ production by peripheral blood mononuclear cells (PBMC), mediated by IFN-α/β. ODN 2216 activates NK cells and induces IFN-γ production by TCR-triggered CD4+ T 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.

PD-1 PD-L1-IN-31 is a potent inhibitor of PD-1 PD-L1 (IC50=2.2 nM) that enhances IFN-γ secretion and activates the immune response of peripheral blood mononuclear cells (PBMCs), leading to the inhibition of tumor cells [1].

Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) serves as a T cell proliferation activator by promoting the dose-dependent in vitro proliferation of human peripheral blood mononuclear cells (PBMC) and is used in research on inflammation, immunity, and cancer [1].

ODN D-SL03, a class C CpG oligonucleotide, effectively stimulates peripheral blood mononuclear cells (PBMCs) to produce high levels of IFN-α. It activates human B cells, NK cells, and mononuclear cells, elevating the expression of CD80, CD86, and HLA-DR on PBMC subsets' surface. Additionally, ODN D-SL03 impedes tumor growth. Its sequence: 5'-tcgcgaacgttcgccgcgttcgaacgcgg-3' [1].

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

STING modulator-5 (compound 38), a STING modulator, exhibits a pIC50 value of 9.5 and antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. Additionally, it acts as an antagonist of THP-1 cells, making it applicable in immunological disease research [1].

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

LEO 39652, a dual-soft PDE4 inhibitor, demonstrates potent inhibition of PDE4 subtypes A, B, C, and D with respective IC50 values of 1.2 nM, 1.2 nM, 3.0 nM, and 3.8 nM. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM, indicating its potential for topical Atopic dermatitis (AD) research [1].

PROTAC IRAK4 Degrader-2 (Compound 9) is a PROTAC-based degrader that potently reduces IRAK4 levels, achieving a DC50 of 151 nM in peripheral blood mononuclear cells (PBMCs). It also notably decreases IRAK4 protein levels with a DC50 of 36 nM in the same cell type and inhibits several cytokines in PBMCs [1].

HPK1-IN-3 is a selective, potent, ATP-competitive inhibitor of hematopoietic progenitor cell kinase 1 (HPK1; MAP4K1) (IC50: 0.25 nM). HPK1-IN-3 has IL-2 cellular potency and is able to act on human peripheral blood mononuclear cells (PBMC) with an EC50 value of 108 nM.

EIF2α activator 2 (Compound 1) is a phosphorylated activator of eukaryotic initiation factor 2α (eIF2α), exhibiting anti-proliferative effects in K562 cells (IC50: 4.79 μM) and PBMC cells (IC50: 10.52 μM).