SML2097
Lys05
≥98% (HPLC)
别名:
Lys-01 3HCl, Lys-05, Lys01 3HCl, N-（7-氯喹啉-4-基）-N′-[2-[（7-氯喹啉-4-基）氨基]乙基]-N′-甲基乙烷-1,2-二胺三盐酸盐, N1-（7-氯喹啉-4-基）-N2-[2-[（7-氯喹啉-4-基）氨基]乙基]-N2-甲基乙烷-1,2-二胺三盐酸盐, PS-1001, PS1001
InChI key
JTUYDBHQGOZPQQ-UHFFFAOYSA-N
SMILES string
[Cl-].[Cl-].[Cl-].Clc1cc2nccc(c2cc1)[N+H2]CC[N+H](CC[N+H2]c3c4c(ncc3)cc(cc4)Cl)C
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Application
Lys05已被用作自噬抑制剂来研究其与哌嗪的相互作用。它也被用作溶酶体抑制剂，以研究其对Gallus gallus肌肉发生的影响。
Biochem/physiol Actions
Lys05（Lys01三盐酸盐）是一种二聚氯喹（CQ），可使溶酶体脱酸并导致溶酶体酶受损，其自噬抑制能力比羟氯喹（HCQ）和CQ高10倍以上（LN229胶质母细胞瘤细胞中的10 μM处理4小时后，LC3II/LC3I比=15.4，使用100 μM CQ或HCQ，LC3II/LC3I比=<6.4）。Lys05在体外（在1205Lu，c8161，LN229，HT-29培养物中，HCQ的IC50 3.6-6.0 μM与15.6-23.8 μM）和小鼠体内（降低肿瘤生长速率的EC50∼10 mg/kg/天腹腔注射；HT29异种移植物）也显示出更高的抗癌活性，由于溶菌酶的显著减少，仅在高剂量（≥80 mg/kg）下才观察到毒性。
在体外和体内，二聚氯喹（CQ）具有比羟氯喹（HCQ）和CQ更高的自噬抑制效力。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Kayo M Bagri et al.
BioMed research international, 2020, 6404230-6404230 (2020-07-21)
Lysosomes and acidic compartments are involved in breaking down of macromolecules, membrane recycling, and regulation of signaling pathways. Here, we analyzed the role of acidic compartments during muscle differentiation and the involvement of the Wnt/beta-catenin pathway in lysosomal function during
Valentina Sica et al.
Cell reports, 27(3), 820-834 (2019-04-18)
Inhibition of oxidative phosphorylation (OXPHOS) by 1-cyclopropyl-4-(4-[(5-methyl-3-(3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl)-1H-pyrazol-1-yl)methyl]pyridin-2-yl)piperazine (BAY87-2243, abbreviated as B87), a complex I inhibitor, fails to kill human cancer cells in vitro. Driven by this consideration, we attempted to identify agents that engage in synthetically lethal interactions with B87. Here, we
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