mononuclear

(S)-(+)-Rolipram ((+)-Rolipram) 是一种 cAMP 依赖性磷酸二酯酶 4 (PDE4) 抑制剂，IC50=1100 nM。它能够抑制人单核细胞产生的肿瘤坏死因子 α (TNFα)。

Gardiquimod 可抑制巨噬细胞和活化的外周血单个核细胞的HIV-1感染。 它是一种咪唑喹啉类似物，是一种 TLR7 8 激动剂。

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。

Amlexanox (AA673) 是一种特异性的 IKKε和 TBK1抑制剂，其 IC50=1-2 μM。

AZD-4877 是一种高效的纺锤体驱动蛋白 (Eg5) 抑制剂，对其 IC50 值为 2 nM。 AZD-4877 是 Ispinesib 的另一种构型， 能够抑制细胞有丝分裂，诱导形成单极纺锤体表型，介导细胞凋亡(Apoptosis)。 AZD-4877 具有抗肿瘤活性，对循环外周血单核细胞 (PBMC)有抑制作用。

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。

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.

Manumycin A 是一种具有抗癌活性的抗生素，是哺乳动物硫氧还蛋白还原酶-1 （TrxR-1） 抑制剂。Manumycin A 以剂量依赖性方式抑制 TNF α 刺激的 THP-1 细胞和外周血单核细胞中 IL-1β 、IL-6 和 IL-8 的产生，诱导细胞凋亡。

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。

Lenacapavir，又名GS-6207，是一种HIV-1 capsid抑制剂。其对23种来自不同亚型的HIV-1临床分离株表现出平均EC50为50 pM (20-160 pM)，这些测试是在周围血单核细胞（PBMCs）中进行的。Lenacapavir在体外显示出皮克摩尔级的有效性，且对现有抗逆转录病毒类化合物没有交叉抗性。此外，在HIV-1感染者中，Lenacapavir展现出强大的抗病毒活性，无论治疗历史如何，都没有发现对Lenacapavir的预存在抗性。

Gardiquimod (hydrochloride) 是一种咪唑啉类的TLR7 8激动剂。它能够抑制巨噬细胞和激活外周血单个核细胞 (PBMCs) 的HIV-1感染。当浓度低于10 μM时，Gardiquimod (hydrochloride) 可以特异性地激活TLR7。

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。

5-Et-ddU, Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells.

CK176 is a capsid targeted inhibitor of HIV-1 replication. CK176 shows an 11-fold improvement over I-XW-053 in blocking HIV-1 replication in primary human peripheral blood mononuclear cells (PBMCs).

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).

SMU127 is an agonist of the toll-like receptor 1 2 (TLR1 2) heterodimer.1It induces NF-κB signaling in cells expressing human TLR2 (EC50= 0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM.In vivo, SMU127 (0.1 mg animal) reduces tumor volume in a 4T1 murine mammary carcinoma model. 1.Chen, Z., Cen, X., Yang, J., et al.Structure-based discovery of a specific TLR1-TLR2 small molecule agonist from the ZINC drug library databaseChem. Commun. (Camb.)54(81)11411-11414(2018)

O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral administrationXenobiotica41(12)1063-1075(2011) 2.Lu, Y., Shen, X., Hang, T., et al.Identification and characterization of process-related substances and degradation products in apremilast: Process optimization and degradation pathway elucidationJ. Pharm. Biomed. Anal.14170-78(2017) 3.Bhole, R.P., Naksakhare, S.R., and Bonde, C.G.A stability indicating HPTLC method for apremilast and identification of degradation products using MS MSJ. Pharm. Sci. & Res.11(5)1861-1869(2019)

p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells.

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