CUR5g

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CUR5g 是一种有效的自噬 (autophagy) 抑制剂。CUR5g 通过阻断自噬体-溶酶体融合选择性地抑制癌细胞中的自噬体降解。CUR5g 通过依赖 UVRAG 的机制阻止 STX17 募集到自噬体，导致自噬体无法与溶酶体融合。CUR5g 可提高顺铂 (Cisplatin，HY-17394) 在体外和体内对 A549 细胞的抗癌作用。

CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo.

Cell Autophagy AssayCell Line:A549 cellsConcentration:0, 1, 5, 10, 20, and 40 μM Incubation Time:3, 6, 12, and 24 h Result:Induced extensive cytoplasmic vacuolization, and GFP-LC3B signal shifted from diffuse cytosolic staining to a punctate pattern outlining autophagosomes.Western Blot Analysis Cell Line:A549 cells Concentration:0, 1, 5, 10, 20, and 40 μM Incubation Time:0, 1, 3, 6, 12, and 24 h Result:Up-regulated LC3B-II and sequestosome 1 (SQSTM1) levels time- and dose-dependently. This increase was not the result of enhanced transcription, as mRNA expression of SQSTM1 and LC3B were not increased within CUR5g-exposed cells, suggesting that CUR5g might block autophagic flux rather than increase autophagosome formation.Cell Proliferation Assay Cell Line:A549 cells Concentration:0, 1, 5, 10, 20, and 40 μM Incubation Time:24 h Result:Exhibited great toxicity to A549 cells at 20 μM. Slightly decreased A549 cell number at 10 μM, while decreased the number of A549 cells significantly at 20 μM. Showed no discernable activity in healthy human umbilical vein endothelial cell (HUVEC) viability at 40?μM.

Animal Model:BALB/c nude mice (4-week-old, A549 cells were subcutaneously injected into the right scapula of each nude mouse)Dosage:40?mg/kg, CUR5g (40 mg/kg) and Cisplatin (1 mg/kg) Administration:Injected via caudal vein, once every 2 days for up to 15 days Result:Retarded the growth of xenografted tumors, whereas the combination treatment with Cisplatin almost completely inhibited tumor growth. Promoted the cisplatin sensitivity of A549 cells by inhibiting autophagic flux.

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Autophagy

Autophagy

Autophagy

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1370032-20-4

344.41

C22H20N2O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 41.67 mg/mL (120.99 mM; 超声助溶 (<60°C)

C(\C=1C=2C(NC1)=CC=CC2)=C\3/C(=O)\C(=C\C4=CC=C(O)C=C4)\CN(C)C3

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(-20℃)

With Ice Pack

≥ 2 years