PBMC cells

BC-1215 是一种 F-box protein 3 抑制剂。它能够稳定 TRAF1-TRAF6 来抑制 Fbxo3-TRAF 激活途径。它与 ApaG 相互作用，阻碍来自人 PBMC 广谱 TH1 细胞因子的分泌。

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) 是细胞天然免疫中第二信使，在 DNA 结合条件下由 cGAMP 合成酶 (cGAS) 催化形成。2',3'-cGAMP sodium 可与 STING 结合形成二聚体，诱导 IFN-β 及其他细胞因子的产生和表达。

Fludarabine (Fludarabinum) 是一种氟化嘌呤类似物，一种核酸合成抑制剂和 STAT1 激活抑制剂。Fludarabine 具有抗肿瘤活性，可以用于治疗白血病和淋巴瘤。

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂，其在人和小鼠中的 EC50 值分别为 130 nM 和 186 nM。。

Rifampicin (Rifamycin AMP) 是一种广谱抗生素。Rifampicin 对结核杆菌有较强抗菌作用，对革兰氏阳性或阴性细菌、病毒等也有疗效。

Vicriviroc maleate (SCH-417690 (maleate)) 是一种可口服，可透过血脑屏障的 CCR5选择性拮抗剂，同时抑制外周血单核细胞中的 HIV-1 的活性。

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。

Emtricitabine 是一种核苷逆转录酶抑制剂， 具有抗人类免疫缺陷病毒 （HIV） 和乙型肝炎病毒的活性,在 PBMC 细胞中的 EC50值为0.01 µM，可用于研究 HIV 感染。

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 作为LRRK2抑制剂，展现出显著的抑制活性。该化合物在PBMC细胞中的IC50值仅为5 nM，而对BCRP的IC50值则为1.5 μM，表明其选择性抑制效果。LRRK2-IN-15 主要用于帕金森病相关研究。

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。

JTE-607 HCl 是高选择性的炎性细胞因子合成抑制剂，可保护小鼠免受内毒素休克。它作用于 LPS 刺激的人 PBMC，抑制TNF-α(IC50:11 nM)、IL-1β(IC50:5.9 nM)、IL-6(IC50:8.8 nM)、IL-8(IC50:7.3 nM)和IL-10(IC50:9.1 nM)。

Kaempferitrin (Lespenephryl) 是天然黄酮苷类化合物，具有缓解疼痛、抗糖尿病、消炎、抗肿瘤和化疗作用，可激活胰岛素信号传导。

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 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1]. LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin[2]. LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin[1].Pharmacokinetic AnalysisLEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 300 mL min kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg kg)[1]. [1]. Jens Larsen, et al. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3 H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5- a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel Dual-Soft PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis. J Med Chem. 2020 Dec 10;63(23):14502-14521.[2]. Stefan Eirefelt

Indinavir sulfate (L735524 sulfate) 是一种 HIV 蛋白酶抑制剂。它抑制 HIV-1 蛋白酶，IC50 值为 0.41 nM，Ki 值为 0.24 nM。它也是SARS-CoV 3CLpro 抑制剂，IC50为 1.71 μM。

EIF2α activator 2（Compound 1）是一种真核生物起始因子2α（eIF2α）磷酸化的激活剂。EIF2α 激活剂 2 在 SRB 细胞增殖试验中表现出高效力 (IC50: 0.46 μM)。EIF2α activator 2 对 K562 (IC50: 4.79 μM)和 PBMC (IC50: 10.52 μM) 细胞表现出抗增殖活性。

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。

EIF2α activator 1（Compound 40）为真核生物起始因子2α（eIF2α）磷酸化的激活剂，能够提高EIF2α下游蛋白ATF和CHOP的表达水平。该化合物对K562细胞和PBMC细胞展现出抗增殖活性，其IC50值分别为4.00 μM和19.3 μM。

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).

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。

STINGmodulator-5（compound 38）为THP-1和外周血单个核细胞（PBMC）的拮抗剂，其在THP-1上的pIC50值为8.9，在PBMC上的pIC50值为8.1。此化合物适用于免疫性疾病研究。