endocytosis

Pitstop2 是一种两性蛋白结合的网格蛋白末端结构域抑制剂 (IC50=12 μM)，具有选择性。 Pitstop2 严重干扰受体介导的内吞作用、HIV 进入和突触小泡循环。Pitstop 2 具有抗肿瘤活性。

Clathrin-IN-1 是一种网格蛋白抑制剂，可通过与网格蛋白的末端域相关联来抑制网格蛋白介导的内吞作用，有潜力用于抗癌的研究。

ES9-17 是网格蛋白介导的内吞作用 (CME)的抑制剂。 CME 是植物胞外环境中质膜蛋白和分子内化的主要途径。ES9-17 抑制FM4-64和转铁蛋白的摄取。ES9-17 可以抑制拟南芥 (Arabidopsis) 幼苗的根生长。

Hydroxy-Dynasore (Dyngo-4a) 是 Dynasore 结构模拟类似物，是一种改进的，低细胞毒性的 dynamin 通用抑制剂，抑制 dynamin 依赖性转铁蛋白的内吞作用的 IC50为 5.7 μM，对大脑重组 dynamin I 和重组鼠 dynamin II 的 IC50值分别为 0.38 μM 和 2.3μM。

Ikarugamycin, an antibiotic, is an inhibitor of clathrin-mediated endocytosis (CME).

Amivantamab (JNJ-61186372) 是一种人源可识别表皮生长因子受体 （EGFR） 和 MET 原癌基因 （MET）的抗体，具有抗癌抗肿瘤活性，可防止配体与 EGFR 和 MET 结合以及抑制下游信号转导的受体二聚化。Amivantamab 可诱导巨噬细胞的 Fc 依赖性胞吞作用和自然杀伤细胞的抗体依赖性细胞毒性，可用于研究转移性非小细胞肺癌。

Dynamin IN-2是一种Wiskostatin 类似物。Dynamin IN-2有效抑制 dynamin ，对 dynamin I GTPase 的 IC50 为 1.0 μM。Dynamin IN-2 可阻断网格蛋白介导的内吞作用 (CME)，IC50 为 9.5 μM。

Barbadin 是一种新型且具有特异性的 β-arrestin β2-adaptin 相互作用抑制剂，对β-arestin1 的 IC50 值为 19.1 μM，对β-arestin2 的 IC50 值为 15.6 μM。Barbadin 增强氯卡色林对 POMC 神经元和减肥的长期影响，可阻断激动剂促进的原型 β2-肾上腺素能、V2-血管加压素和血管紧张素-II-1 型受体的内吞，可用于研究肥胖。

UNI418是一种具备抗SARS-CoV-2病毒活性的PIKfyve和PIP5K1C双抑制剂，其EC50值为1.4 μM。该化合物通过抑制PIP5K1C (IC50为60.1 nM; Kd为61 nM)来阻断ace2介导的病毒内吞作用。同时，UNI418抑制了由PIKfyve调控 (Kd为0.78 nM)，关键于SARS-CoV-2病毒进入宿主细胞的蛋白酶的蛋白水解活化。

AAK1 HDACs-IN-1 (Compound 12) 是一种同时抑制AAK1和HDAC的化合物，能够对AAK1、HDAC1和HDAC6产生抑制作用，其IC50值分别是15.9、148.6和5.2 nM。它可以抑制SARS-CoV-2感染，通过抑制ACE2-SARS-CoV-2复合物的内吞作用以及AP2M1-ACE2之间的相互作用实现。

Dynole 34-2(Dynamin Inhibitor V, 34-2)是一种强效和非竞争性的的dynamin1和dynamin2 GTPase抑制剂，通过靶向GTPase结构域的变构位点，抑制受体介导的内吞作用和突触囊泡内吞作用。Dynole 34-2在多种细胞系中表现出抗有丝分裂作用，诱导细胞凋亡。

BMS-986176 是一种有效的AAK1 抑制剂，IC50为 2.2 nM。BMS-986176在神经退行性疾病中有研究的价值。

Cho-Arg is a steroid-based cationic lipid that contains a cholesterol skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratios greater than or equal to 4. Cho-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence or absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It is cytotoxic to H1299 cells (IC50 = 88.5 μg/ml).

Dios-Arg is a steroid-based cationic lipid that contains a diosgenin skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratio greater than or equal to 4. Dios-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence and absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It has been used, coupled to 1,2-dioleoyl-sn-glycero-3-PE , to bind siRNA and plasmid DNA to form cationic lipid nanoparticles for intracellular transport. Dios-Arg is cytotoxic to H1299 and HeLa cells (IC50s = 83.5 and 74.1 μg/ml, respectively).

2H-Cho-Arg is a steroid-based cationic lipid that contains a 2H-cholesterol skeleton coupled to an L-arginine head group and can be used to facilitate gene transfection. It forms a complex with plasmid DNA (pDNA) and decreases pDNA migration in an electrophoretic mobility shift assay at +/- charge ratios of 4 or higher. 2H-Cho-Arg facilitates transfection of a luciferase gene into H1299 cells, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein , but not by inhibitors of clathrin- or micropinocytosis-mediated endocytosis. It induces cytotoxicity in H1299 cells (IC50 = 92.7 μg/ml).

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).

RTIL 13 is a highly effective inhibitor of dynamin GTPase, exhibiting an IC50 value of 2.3 μM for dynamin I GTPase. Furthermore, it selectively interacts with the pleckstrin homology lipid binding domain. This compound effectively suppresses both receptor-mediated and synaptic vesicle endocytosis, demonstrating IC50 values of 9.3 μM and 7.1 μM, respectively.

Biotin-TAT (47-57) is a biotin-tagged transactivator of transcription, commonly employed as a protein transduction domain (PTD) in various primary cells. Its transduction capacity is contingent on ATP and temperature, suggesting the participation of endocytosis.

Dynole 2 24 是一种基于吲哚的dynamin GTPase 抑制剂 (对 dynamin I 的IC50=0.56 μM)。Dynole 2 24 无毒，在体外和细胞内显示出增强的抗动力蛋白I 和II 的效力 (IC (CME)=1.9 μM)。Dynole 2 24 对 dynamin I 的选择性为4.4倍。Dynole 2 24在网格蛋白介导的内吞作用的细胞抑制剂中具有活性。CME: Clathrin mediated endocytosis

PD-1 PD-L1-IN-14 (compound 17) 是PD-1 PD-L1相互作用的抑制剂（IC50= 27.8 nM）。通过抑制PD-1 PD-L1 相互作用，PD-1 PD-L1-IN-14促进二聚化，内吞作用并降解 PD-L1。

[Tyr3]Octreotate 是一个含有8个氨基酸的长肽化合物，是具有共价键DOTA 双功能螯合剂。[Tyr3]Octreotate 与SSR2活性的NETs 的跨膜受体结合，并通过内吞作用主动运输到细胞中，可能会增加所需的双链DNA 断裂，是治疗肿瘤的潜在药物。

Clathrin-IN-2 是网格蛋白介导的内吞作用(CME)的有效抑制剂，IC50值为 2.3 μM。 Clathrin-IN-2 还对dyn I GTPase 具有抑制作用，IC50值为 7.7 μM。

Dynamininhibitory peptide TFA 竞争性地阻止了动力蛋白 (dynamin) 与两性纤维蛋白的结合，从而防止了内吞作用。Dynamininhibitory peptide TFA 阻断多巴胺 D3对 GABAA 受体的作用。

Neurokinin Receptor(393-407), rat (SPR393–407) 是一段属于大鼠神经激肽1受体(NK1R)的特定肽。它与P物质(SP)结合后，通过内吞作用迅速被NK1R内化，并循环至质膜。此化合物主要应用于神经源性炎症研究领域。