PBMCs

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]

Gardiquimod is a TLR7/8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

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

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.

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.

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

Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).

Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

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

Mapracorat (ZK-245186, BOL-303242X) is a selective glucocorticoid receptor agonist commonly used as an anti-inflammatory agent for atopic dermatitis, post-cataract surgery inflammation, and allergic conjunctivitis.

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.

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

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).

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).

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.

Robinin (NSC-9222) belongs to natural products, serving as a TLR2 inhibitor with cell permeability. Robinin exerts anti-inflammatory and antitumor activities through inhibiting the TLR2-PI3K-AKT pathway, and can be used for experimental research related to pancreatic cancer.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

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 (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.

HPK1-IN-56 (Compound A29) is an HPK1 inhibitor with an IC50 of 2.70 nM. It inhibits downstream p-SLP76 in Jurkat T cells with an IC50 of 8.1 nM. Additionally, HPK1-IN-56 induces IL-2 production in human PBMCs. This compound exhibits anticancer properties, enhancing T cell cytotoxicity and the antitumor efficacy of anti-PD-1 antibodies.

STF-1084 is an inhibitor that cannot penetrate cells and targets ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1) with an apparent Ki of 0.11 µM. It demonstrates selectivity for ENPP1 over ENPP2 and alkaline phosphatase (ALP) with apparent Kis of 5.5 and >100 µM, respectively, and does not affect a panel of 468 kinases at 1 µM. STF-1084 hinders the extracellular breakdown of cGAMP in ENPP1-overexpressing and cGAS-expressing 293T cells, with an IC50 of 0.340 µM, and enhances mRNA expression for the gene encoding IFN-β in CD14+ primary human peripheral blood mononuclear cells (PBMCs) when incubated with conditioned medium from ENPP1-overexpressing and cGAS-expressing 293T cells treated with STF-1084. In a live setting, STF-1084, when combined with ionizing radiation, elevates the proportion of tumor-associated CD11c+ cells among antigen-presenting cells (APCs) in a murine mammary cancer model (4T1).

diABZI-a1 is an orthogonal STING agonist with an EC50 of 117 nM for inducing IFNβ in human PBMCs. This compound is applicable in the study of monogenic autoinflammatory diseases such as SAVI disease.

diABZI-i functions as an orthogonal STING inhibitor, significantly suppressing cGAMP-induced IFNβ in PBMCs with an IC50 of 49 nM. Additionally, diABZI-i activates V155M SAVI constitutive signaling in a STINGV155M THP-1 cell model, demonstrating potent agonistic activity (EC50: 17 nM). This compound is applicable in researching monogenic autoinflammatory diseases such as SAVI.