electrophilic

Cysteine thiol probe (Methyl (4-bromobenzoyl)-L-cysteinate) 是基于硫醇的探针，旨在标记亲电子的天然产物。它能够结合基于烯酮，β-内酰胺和 β-内酯的亲电子代谢物。它具有理想药效团探针的每个特征，并具有发色团。

α-Angelica lactone 是一种乙烯基亲核试剂，也是一种天然存在的抗癌剂。它可以得到手性的 δ-氨基 γ，γ-二取代丁烯醇内酯羰基衍生物，并在 γ-碳上表现出亲电子俘获。它通过选择性增强谷胱甘肽-S-硫转移酶 (GST) 和 UDP-葡糖苷转移酶 (UGT) 解毒酶发挥强大的化学保护作用。

PF4840154 是有效的大鼠和人TrpA1通道选择性激动剂，EC50分别为 97 和 23 nM。PF-4840154 可以诱导 TrpA1 介导的小鼠伤害行为。

4-Hydroxycoumarin 是香豆素衍生物，也是通用的杂环支架之一，具有亲电和亲核性质。

6-Bromo-2-naphthol 是一种亲电卡宾(carbene) 中间体。

2-tert-Butyl-1,4-benzoquinone 是丁基化羟基茴香醚 (BHA) 的亲电子代谢物，它在 RAW264.7 细胞中引起 Nrf2 的活化及其负调节剂 Keap1 的 S-芳基化。

DiaAlk is a clickable, electrophilic diazene probe which enables capture and site-centric proteomic analysis of oxidative post-translational modification (OxiPTM).

Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatocellular carcinoma cells when used at a concentration of 4 μM.3 1.Qian-Cutrone, J., Huang, S., Shu, Y.-Z., et al.Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cellsJ. Am. Chem. Soc.124(49)14556-14557(2002) 2.Wulff, J.E., Herzon, S.B., Siegrist, R., et al.Evidence for the rapid conversion of stephacidin B into the electrophilic monomer avrainvillamide in cell cultureJ. Am. Chem. Soc.129(16)4898-4899(2007) 3.Hu, L., Zhang, T., Liu, D., et al.Notoamide-type alkaloid induced apoptosis and autophagy via a P38/JNK signaling pathway in hepatocellular carcinoma cellsRSC Adv.9(34)19855-19868(2019)

Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.2 1.Yamada, T., Iritani, M., Ohishi, H., et al.Pericosines, antitumour metabolites from the sea hare-derived fungus Periconia byssoides. Structures and biological activitiesOrg. Biomol. Chem.5(24)3979-3986(2007) 2.Du, L., Munteanu, C., King, J.B., et al.An electrophilic natural product provides a safe and robust odor neutralization approach to counteract malodorous organosulfur metabolites encountered in skunk sprayJ. Nat. Prod.82(7)1989-1999(2019)

DB008 是一种有效的选择性PARP16抑制剂，IC50值为 0.27 μM，含有丙烯酰胺亲电试剂。DB008 具有膜渗透性，可选择性标记PARP16。

MitoCur-1为一种姜黄素类似物，作为线粒体抗氧化硫氧还蛋白还原酶2（TrxR2）抑制剂，展现亲电性与线粒体靶向特性。该化合物能特异性诱导活性氧（ROS）生成，表现出抗肿瘤活性。

AM841是一种高亲和力的亲电子配体，能与CB1大麻素受体中第六螺旋的半胱氨酸发生共价作用并激活该受体。此外，AM841能减少Forskolin刺激下的cAMP积累，并且减缓胃肠蠕动。

MN551是一种高效的半胱氨酸定位亲电共价键抑制剂，对SOCS2与其CRL5复合物的生物作用及在PROTACs诱导的目标蛋白降解过程中扮演关键角色。

2,6-Dithiopurine (2,6-Dimercaptopurine) 作为一种亲核清除剂，有效消除 DNA 加合物的形成，阻断亲电致癌物的致癌启动过程。

Cyprocide-B在经Cytochrome P450激活后会转变为亲电性代谢物,能特异性地消灭线虫C. elegans.该化合物为开发选择性杀线虫剂提供了研究基础.

2-bromomethyl benzothizaole 是苯并噻唑的衍生物。它是一种中间体和构建块亲电试剂，已被用于合成许多化合物，如2-bromo-4-methyl-1,3-benzothiazole，一种用于合成新型抗真菌剂的化合物。

Biotin-PEAC5-maleimide hydrochloride 是一种用于生物素-PEAC5-马来酰亚胺 (BPM) 标记的生化检测试剂，适用于评估亲电子试剂对蛋白质硫醇的修饰。