mononuclear cell

5J-4 是一种有效的钙释放激活钙通道 (CRAC) 和钙池操纵性钙内流(SOCE) 阻滞剂。 5J-4 减少 IL-17 的产生并降低 RORα 和 RORγt 的表达。

Enpatoran (M5049) 是一种口服有效的TLR7 8选择性抑制剂，在HEK293 细胞中，IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran 在体内具有良好的药代动力学特性。Enpatoran 在先天性和适应性自身免疫阻断方面有研究的价值。

AZD7624 是一种 p38 抑制剂，具有强大的抗炎活性。

MG-T-19是一种TIM-3抑制剂（KD=0.26 μM），显著抑制TIM-3与PtdSer、CEACAM1和Gal-9的相互作用，增加PBMCs中TNF-α和IFN-γ的产生，从而重新激活T细胞对肿瘤的攻击能力。

Rufloxacin hydrochloride (MF-934 hydrochloride) 是一种氟喹诺酮类抗菌剂，可抑制拓扑异构酶。 Rufloxacin hydrochloride 抑制人单核细胞中的 B 细胞分化。

Apoptosisinducer 26 (化合物 [AgCl(dap2SH)(PPh3)2]) 作为一种基于单核 Ag(I) 配体的化合物，展现出针对多种细菌菌株和癌症细胞系的显著抗菌及抗癌活性。该化合物可促使 Ag(I) 离子在细菌的周质中聚集，有效地抑制革兰氏(+)和革兰氏(-)细菌的增长。此外，Apoptosisinducer 26 还能够介入 CT DNA 的碱基对之间，引发 A549 细胞的凋亡过程，并具备清除自由基的功能，有助于防御氧化压力。

4 -C18 EGCG 是一种高效抑制α-淀粉酶和α-葡萄糖苷酶的化合物，其IC50值为3.74和0.81 μM，分别显示出强效。该化合物能够抑制碳水化合物水解酶，减轻氧化应激和炎症，展现出抗糖尿病的潜力。此外，4 -C18 EGCG 还通过下调促炎细胞因子，对原代人外周血单核细胞（PBMC）、非癌细胞系如3T3-L1和HEK 293，显示出高达50 μM的细胞毒性。

4''-C18 EGCG 具备高效的抑制作用，针对α-淀粉酶和α-葡萄糖苷酶，其 IC50 值分别为 3.74 μM 和 0.81 μM。该化合物通过抑制碳水化合物水解酶来降低氧化应激和炎症，展现出抗糖尿病的活性。此外，4''-C18 EGCG 还能下调促炎细胞因子，对原代人外周血单核细胞 (PBMC)、3T3-L1 和 HEK 293 非癌细胞系的细胞毒性为 50 μM。

Myelin Basic Protein (87-99) Acetate (Myelin Basic Protein (87-99) Acetate (118506-26-6 Free base)) 是一种致脑炎肽，可诱导碱性蛋白特异性 T 细胞增殖。 它导致外周血单核细胞中的 Th1 极化，这与多发性硬化症 (MS) 有牵连。

I-XW-053 sodium inhibits the replication of a diverse panel of primary HIV-1 isolates in Peripheral blood mononuclear cell with no appreciable cytotoxicity.

(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).

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

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).

Ganglioside GT1b is a trisialoganglioside that is characterized by having two sialic residues linked to the inner galactose unit. It binds to the neurotoxins botulinum toxin serotype A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively.[1] Ganglioside GT1b-containing liposomes bind to the major coat protein VP1 from Merkel cell polyomavirus (MCPyV), which has been identified in Merkel cell carcinomas, identifying ganglioside GT1b as a putative MCPyV receptor. [2] Ganglioside GT1b decreases production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMCs) by 31.4, 30.5, 60, 59.5, and 58%, respectively, when used at a concentration of 10 μM [3] . Ganglioside GT1b mixture contains ganglioside GT1b molecular species with C18:1 and C20:1 sphingoid backbones.

BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).1 It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 μM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro. |1. Archambault, A.-S., Turcotte, C., Martin, C., et al. Comparison of eight 15-lipoxygenase (LO) inhibitors on the biosynthesis of 15-LO metabolites by human neutrophils and eosinophils. PLoS One 13(8), e0202424 (2018).

Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.

p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively). Laufer et al (2003) Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J.Med.Chem. 46 3230 PMID:12852754 |Kammerer et al (2007) Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor. Drug Metab.Dispos. 35 875 PMID:17344341

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).

HPK1-IN-3 是一种选择性的、有效的、ATP 竞争性的造血祖细胞激酶 1 (HPK1; MAP4K1) 抑制剂 (IC50: 0.25 nM)。HPK1-IN-3 具有 IL-2 细胞效力，能够作用于人外周血单核细胞 (PBMC)，EC50 值为 108 nM。

KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chemokine, stromal cell-derived factor 1alpha, to CXCR4 specifically and subsequent signal transduction. KRH-1636 prevented monoclonal antibodies from binding to CXCR4 without down-modulation of the coreceptor. KRH-1636 seems to be a promising agent for the treatment of HIV-1 infection.

PROTACIRAK4 degrader-2 (Compound 9) 是一种 PROTACIRAK4降解剂，在外周血单个核细胞 (PBMC) 中，降解 IRAK4，DC50为 151 nM。PROTACIRAK4 Degrader-2 在 PBMC 细胞中诱导 IRAK4蛋白水平降低，DC50为 36 nM。PROTACIRAK4 degrader-2 还抑制 PBMC 中多种细胞因子释放。

ICeD-2 是一种细胞死亡诱导剂，可诱导HIV-1感染的细胞死亡。 ICeD-2 介导的HIV-1感染细胞杀伤依赖于HIV-1蛋白酶活性。ICeD-2 可有效阻断二肽基肽酶DPP8和DPP9对 Gly-Pro-AMC 的水解。ICeD-2 显示 PBMC 中 DPP9 的强稳定性。

Myelin Basic Protein(87-99) TFA 为诱导神经碱性蛋白特异性T细胞增殖的致脑肽。该化合物能在外周血单核细胞中诱导Th1极化，与多发性硬化症(MS)的发病机制相关。

FB49是一种针对Bcl-2-associated athanogene 3 (BAG3)的高选择性抑制剂，具有Ki值为45 μM。在人类肿瘤细胞系中，FB49能够有效抑制细胞生长，同时对人外周单核细胞无明显毒性。此外，FB49能够在HD-MB03成神经管细胞瘤细胞中阻碍G1期的细胞周期进程，并诱导细胞凋亡(apoptosis)和自噬(autophagy)。