pbmcs

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

Azithromycin (CP 62993) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.

Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.

Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]

ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.

Cenicriviroc (TAK-652) is an orally active, dual CCR2 CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.

IT1t dihydrochloride inhibits CXCL12 CXCR4 interaction with IC50 of 2.1 nM. IT1t dihydrochloride is an antagonist of CXCR4.

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).

TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.

HPK1-IN-47, a PROTAC HPK1 degrader (DC 50: 23 nM in PBMCs), serves as a precursor for the synthesis of compounds like PROTAC HPK1 Degrader-2. It is utilized in research focused on diseases mediated by HPK1, including cancer.

Lenacapavir, also known as GS-6207, is an HIV-1 capsid inhibitor. It demonstrates an average EC50 of 50 pM (ranging from 20-160 pM) against 23 clinical isolates of HIV-1 from diverse subtypes, with tests performed in peripheral blood mononuclear cells (PBMCs). In vitro, Lenacapavir exhibits picomolar potency and shows no cross-resistance with existing antiretroviral compounds. Furthermore, Lenacapavir displays significant antiviral activity in individuals with HIV-1, regardless of prior treatment history, with no pre-existing resistance detected.

Gardiquimod diTFA, an imidazoquinoline analog and TLR7 8 agonist, inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs), and specifically activates TLR7 at concentrations below 10 μM. As an immune system modifier and reverse transcriptase inhibitor, it serves as a novel therapeutic agent to block systemic and mucosal transmission of HIV-1.[1][2]

M199, a novel inhibitor of TLR3/9 activation, induces secretion of IL-6, IL-8 and TNFalpha in human PBMCs.

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].

Compound A, a potent TLR8 agonist, exhibits an EC50 of 0.052 µM and promotes the production of IL-12p40 in human PBMCs with an EC50 of 0.031 µM. This compound is applicable for research in virus resistance, infection resistance, autoimmunity, and tumor studies [1].

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

Gardiquimod (hydrochloride) is an imidazoquinoline class TLR7 8 agonist. It can inhibit HIV-1 infection in macrophages and activated peripheral blood mononuclear cells (PBMCs). At concentrations below 10 μM, Gardiquimod (hydrochloride) specifically activates TLR7.

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).

BMSpep-57, a potent macrocyclic peptide inhibitor, competitively disrupts the PD-1 PD-L1 interaction, demonstrating a significant inhibitory concentration (IC50) of 7.68 nM. It exhibits binding affinity towards PD-L1 with dissociation constants (Kd) of 19 nM and 19.88 nM in MicroScale Thermophoresis (MST) and Surface Plasmon Resonance (SPR) assays, respectively. This compound enhances T cell functionality by promoting Interleukin-2 (IL-2) production within Peripheral Blood Mononuclear Cells (PBMCs).

d2T, a nucleoside analog of thymidine, exhibits antiviral activity by inhibiting HIV replication in infected human peripheral blood mononuclear cells (PBMCs; EC50 = 0.17 µM). Additionally, 3′-deoxy Thymidine at concentrations of 1, 3, 10, or 30 µM significantly decreases viral plaque formation in CV-1 cells infected with herpes simplex virus 1 (HSV-1).

M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.

IT1t inhibits CXCL12 CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

(+)-Norglaucine shows cytotoxic activity toward the tumor cell lines B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), K562 (human chronic myelocytic leukemia) and HL-60 (human promyelocytic leukemia) and non-tumor peripheral blood mononuc

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).