pbmc cells

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.

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).

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.

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.

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.

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.

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 μM and 0.81 μM respectively. It inhibits carbohydrate-hydrolyzing enzymes, reducing oxidative stress and inflammation, and demonstrates anti-diabetic activity. Additionally, 4 -C18 EGCG downregulates pro-inflammatory cytokines and exhibits cytotoxicity at 50 μM in primary human peripheral blood mononuclear cells (PBMC), and non-cancerous cell lines 3T3-L1 and HEK 293.

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.

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

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.

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].

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.

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).

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 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).

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].

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].