jurkat t

Lifitegrast (SAR 1118) 是一种整合素淋巴细胞功能相关抗原 1 拮抗剂， 抑制 Jurkat T 细胞附着于ICAM-1的IC50为 2.98 nM。

NOTA是一种多功能螯合剂，能够与金属离子形成稳定络合物，常用于放射性药物、分子成像和靶向核治疗。

Soquelitinib(CPI-818)是一种共价，不可逆，可口服和选择性的ITK抑制剂, 优先抑制Th2细胞因子的产生而非Th1，抑制小鼠肿瘤的体内生长，并且降低T细胞衰竭标志物，使正常CD8细胞的肿瘤浸润增加和CXCR3、IFNγ、TNFα和CD107a表达上调。

Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物，可与组胺 H1 受体结合，从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。

Tulipalin A (α-methylene-γ-butyrolactone) 是来源于郁金香鳞茎的有毒糖苷。Tulipalin A 是引起过敏性接触皮炎的致敏性致敏物 (causative allergen)，在低剂量影响免疫细胞的功能，例如 Jurkat T 细胞。

2-Nitrobenzoic acid (o-Nitrobenzoic acid) 是一种抗增殖化合物，对表达 T 型钙通道α1H 或其剪接变体δ25的 jurkat 细胞系显示出8.3μM 的 IC50。

Selinexor (KPT-330) 是一种 CRM1 的小分子抑制剂，具有选择性和口服活性。Selinexor 可以阻滞细胞周期、诱导细胞凋亡，具有抗肿瘤活性，可以用于治疗多发性骨髓瘤。

BMS-1001 hydrochloride 是一种人 PD-L1 PD-1免疫检查点的抑制剂，具有口服活性且细胞毒性低。

15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].

MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂，具有大脑屏障渗透性。

PQA-18 是p21激活激酶2（PAK2；IC50 = 10 nM）的有效抑制剂，并作为Ppc-1（产品编号42352）衍生物展现出免疫抑制特性。该化合物能够降低由刀豆A（产品编号14951）刺激的Jurkat T细胞中IL-2的生成（IC50 = 400 nM）。在应用0.1% PQA-18的情况下，NC Nga小鼠模型显示异位性皮炎的严重程度、血清IgE水平及皮肤厚度有所减轻。此外，0.05%的剂量可有效减少该小鼠模型中皮肤神经纤维的密度。PQA-18（4 mg kg）还在大鼠小肠移植模型中显著提高了移植物的存活率。

HPK1-IN-56 (Compound A29) 是一种HPK1抑制剂，IC50为2.70 nM，抑制下游 p-SLP76 在Jurkat T细胞中的IC50为8.1 nM。此外，HPK1-IN-56 能诱导人PBMCs中IL-2的产生，并表现出抗癌作用，提升T细胞的杀伤能力及增强抗PD-1抗体的抗肿瘤功效。

PD-L1 HDAC6-IN-1 (Compound HP29) 是一种同时抑制PD-L1和HDAC6的化合物，具有抑制PD-L1 PD-1相互作用和HDAC6活性的能力，IC50分别为26.8 nM和69 nM。该化合物增强了Jurkat T细胞对HepG2细胞的杀伤效能，IC50为3.4 μM。在大鼠体内，PD-L1 HDAC6-IN-1展示了良好的药代动力学特征，药物暴露度为871.62 ng·h mL，并且在小鼠B16-F10异种移植模型中表现出抗肿瘤活性。

PD-1/PD-L1-IN-49（compound 1c）是一种高效的PD-1/PD-L1抑制剂，其IC50为77 nM。该化合物能够激活Jurkat T细胞，有效阻断PD-1/PD-L1免疫检查点。

SP-100030 是一种有效的 NF-κB 和激活蛋白-1 (AP-1) 双抑制剂 (IC50 分别为 50 和 50 nM)。SP-10003 抑制 Jurkat 和其他T 细胞系产生的 IL-2、IL-8 和 TNF-α 的产生。SP-100030 降低小鼠胶原性关节炎 (CIA)。

CTA 056 是白细胞介素-2 诱导的 T 细胞激酶（ITK）抑制剂，抑制小鼠 MOLT-4 异种移植肿瘤的生长，诱导 Jurkat 细胞凋亡，可用于研究自身免疫性疾病和T细胞恶性肿瘤。

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human umbilical vein endothelial cells with an IC50value of 56.4 ng/ml.1It induces oxidative stress, DNA damage, and autophagy in, as well as halts the development of, cultured mouse embryos when used at a concentration of 10 nM.3HT-2 toxin has been found in cereal grains and food products.4,5 1.Nielsen, C., Casteel, M., Didier, A., et al.Trichothecene-induced cytotoxicity on human cell linesMycotoxin Res.25(2)77-84(2009) 2.Nathanail, A.V., Varga, E., Meng-Reiterer, J., et al.Metabolism of the fusarium mycotoxins T-2 toxin and HT-2 toxin in wheatJ. Agric. Food Chem.63(35)7862-7872(2015) 3.Zhang, L., Li, L., Xu, J., et al.HT-2 toxin exposure induces mitochondria dysfunction and DNA damage during mouse early embryo developmentReprod. Toxicol.85104-109(2019) 4.Langseth, W., and Rundberget, T.The occurrence of HT-2 toxin and other trichothecenes in Norwegian cerealsMycopathologia147(3)157-165(1999) 5.Al-Taher, F., Cappozzo, J., Zweigenbaum, J., et al.Detection and quantitation of mycotoxins in infant cereals in the U.S. market by LC-MS/MS using a stable isotope dilution assayFood Control72(Part A)27-35(2017)

Padanamide A is a bacterial metabolite originally isolated from a marine Streptomyces species. It is active against five strains of P. falciparum (EC50s = 160-340 nM), is not cytotoxic to HEK293 or HepG2 human cell lines, but is cytotoxic to Jurkat T lymphocytes with an IC50 value of approximately 60 μg/ml.

Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2 M phase. Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation. [2] Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg kg every other day.[1]

CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Kocik, J., et al.Di-bromo-based small-molecule inhibitors of the PD-1/PD-L1 immune checkpointJ. Med. Chem.63(19)11271-11285(2020)

Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but has a low therapeutic index against cancer xenografts when tested in mice.

4-Maleimidosalicylic acid is a polar maleimide compound that does not exhibit suppressive effects on IL-2 production in JURKAT T cells.

Nelarabine (GW 506U78) 是一种嘌呤核苷酸类似物，为DNA 合成抑制剂，对肿瘤细胞的IC50为0.067-2.15 μM，可作用于T 细胞急性淋巴细胞白血病。