e-64

E-64 (Proteinase inhibitor E 64)是一种不可逆的半胱氨酸蛋白酶抑制剂，抑制papain 的IC50为 9 nM。

GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).

NSC-5844 (RE-640) 是 4-氨基喹啉衍生物，起抗肿瘤和抗疟疾作用。

Bunazosin Hydrochloride (E 1015) 是一种 α(1)-adrenoceptor 拮抗剂，用作全身性抗高血压药和降眼压药。

CLIP 86-100 acetate(648881-58-7 free base) 这是称为 CLIP 的 II 类相关不变链肽的氨基酸 86 至 100 片段。主要组织相容性复合物 II 类分子显示外源蛋白的肽片段，以触发免疫系统的防御反应。在将外源肽插入结合槽之前，去除一个占位肽 CLIP。这是通过分子 DM 实现的，它被证明可以增加 CLIP 肽与 II 类的解离速率。

E 64c (EP 475) 是一种不可逆且可透过膜的半胱氨酸蛋白酶抑制剂，是 E-64 的衍生物。它也是钙离子激活中性蛋白酶抑制剂和组织蛋白酶 C 弱不可逆抑制剂，可抑制 MERS-CoV。

E64FC26 是一种有效的蛋白质二硫键异构酶 (PDI) 家族泛抑制剂，具有抗肿瘤活性，抑制 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6，可用于研究多发性骨髓瘤和胰腺癌。

TAE648 是 PROTAC 靶蛋白配体 (Ligand for Target Protein for PROTAC)，可用于合成 PROTAC SK-3-91。

Cariporide (HOE-642) 是一种选择性的Na+/H+交换抑制剂。

Cariporide Mesylate is a selective inhibitor of the Na+/H+ exchanger isoform 1.

(E/Z)-E64FC26 是一种高效的蛋白质二硫键异构酶 (PDI) 家族抑制剂，具有潜在的抗肿瘤活性，对 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6 有亲和力。(E/Z)-E64FC26 可用于研究骨髓瘤。

E6446 dihydrochloride 是一种新型合成拮抗剂，用于核酸感应 TLR；有效抑制对 HEK:TLR9 细胞的 DNA 刺激，IC50 为 10 nM。

E6446 抑制 Toll 样受体 (TLR)7 和 9 信号传导。 E6446 在多种人和小鼠细胞类型中起作用，并在体外抑制 DNA-TLR9 相互作用。当给予小鼠时，该化合物抑制对刺激 TLR9 的含有胞苷-磷酸-胍 (CpG) 的 DNA 的挑战剂量的反应。

Aloxistatin (E64d) 是一种不可逆的、可透过膜的溶酶体和细胞溶质半胱氨酸蛋白酶抑制剂，能够抑制完整血小板中的钙蛋白酶活性。它是一种半胱氨酸蛋白酶抑制剂，具有血小板聚集抑制活性。

EP 459 is a thiol and calpain protease inhibitor.

Arylsulfonamide 64B (HIF inhibitor 64B) 作为一种有效的缺氧诱导因子 (hypoxia induced factor, HIF) 抑制剂，通过抑制缺氧/HIF 诱导的 c-Met 和 CXCR4 的表达，能显著降低葡萄膜黑色素瘤小鼠模型中原发肿瘤的生长与转移。

HAE acetate(64111-99-5 free base) 是由组氨酸、丙氨酸和谷氨酸组成的3个氨基酸肽。

LtaS-IN-1 是多药耐药粪肠球菌中脂磷壁酸合成的有效抑制剂，可改变细胞壁形态。 LtaS-IN-1 对抗肠球菌属 28 菌株，MIC 值从 0.5 μg/mL 到 64 μg/mL 不等。 LtaS-IN-1 抑制菌株 E1630 和 E1590，MIC 值为 0.5 μg/mL。

DNA ligase-IN-2 (compound 2) 是 LigA 的高效抑制剂，能够抑制全长 LigA 及截短酶 LigA:AD 的 DNA 非依赖性自发腺苷酸化活性，其 IC50 为 29 nM。此化合物显著抑制金黄色葡萄球菌的体外生长，对于金黄色葡萄球菌 (S. aureus) ATCC 29213、金黄色葡萄球菌 (S. aureus) ATCC 700699 的 MIC 值为 1 μg/mL，而对大肠杆菌 (E. coli) ATCC 25922 的 MIC 值大于 64 μg/mL。

Antiangiogenic agent 8 (Compound 3m) 是一种抑菌剂，并具有抗血管生成活性。其对E. coli、P. aeruginosa、B. subtilis、S. aureus、C. glabrata的MIC分别为16、8、4、16、8 μg/mL，MBC范围为32-64 μg/mL。Antiangiogenic agent 8 可能在抗感染和心血管疾病研究中具有应用潜力。

Antibacterialagent (compound 8b) 是一种有效的抗菌剂，对E. coli和S. aureus具有显著的抑菌效果，其IC50分别为64 µg/mL和32 µg/mL。

Resolvin E2 (RvE2) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acidviaan 18-HEPE intermediate, which is formed by aspirin-acetylated COX-2-mediated oxidation of EPA, by 5-lipoxygenase (5-LO) in human polymorphonuclear (PMN) neutrophils.2,3RvE2 (20 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of peritonitis induced by zymosan A .3Hepatic RvE2 levels are increased in mice fed normal chow, as well as in a mouse model of high-fat diet-induced non-alcoholic fatty liver disease (NAFLD), by dietary supplementation with EPA.4Plasma levels of RvE2 are increased by dietary supplementation with fish oil containing ω-3 polyunsaturated fatty acids (PUFAs) in patients with peripheral artery disease or chronic kidney disease.1,5,6 1.Chiang, N., and Serhan, C.N.Specialized pro-resolving mediator network: An update on production and actionsEssays Biochem.64(3)443-462(2020) 2.Tjonahen, E., Oh, S.F., Siegelman, J., et al.Resolvin E2: Identification and anti-inflammatory actions: Pivotal role of human 5-lipoxygenase in resolvin E series biosynthesisChemistry & Biology131193-1202(2006) 3.Sungwhan, F.O., Pillai, P.S., Recchiuti, A., et al.Pro-resolving actions and stereoselective biosynthesis of 18S E-series resolvins in human leukocytes and murine inflammationJ. Clin. Invest.121(2)569-581(2011) 4.Echeverría, F., Valenzuela, R., Espinosa, A., et al.Reduction of high-fat diet-induced liver proinflammatory state by eicosapentaenoic acid plus hydroxytyrosol supplementation: Involvement of resolvins RvE1/2 and RvD1/2J. Nutr. Biochem.6335-43(2019) 5.Ramirez, J.L., Gasper, W.J., Khetani, S.A., et al.Fish oil increases specialized pro-resolving lipid mediators in PAD (the OMEGA-PAD II trial)J. Surg. Res.238164-174(2019) 6.Barden, A.E., Shinde, S., Burke, V., et al.The effect of n-3 fatty acids and coenzyme Q10 supplementation on neutrophil leukotrienes, mediators of inflammation resolution and myeloperoxidase in chronic kidney diseaseProstaglandins Other Lipid Mediat.1361-8(2018)

L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitorsBioorg. Med. Chem. Lett.24(1)61-64(2014)

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1]. AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC50=64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC50 60.5 μM against Jurkat cells, and all other CC50 values greater than the highest concentrations tested (25 μM or above)[1].AN3661 inhibits the stability of P. falciparum transcripts[1]. AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED90 (4 days) 0.34 mg/kg[1].AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED90 4 days after initiation of treatment is 0.57 mg/kg[1]. Animal Model: P. berghei-infected mice (malaria model)[1] [1]. Sonoiki E, et al. A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue. Nat Commun. 2017;8:14574. Published 2017 Mar 6.