ZZW-115 hydrochloride |
| Catalog No.GC61393 |
Le chlorhydrate de ZZW-115 est un puissant inhibiteur de NUPR1, avec un Kd de 2,1 μM. Le chlorhydrate de ZZW-115 induit la mort des cellules tumorales par nécroptose et apoptose. Activité anticancéreuse.
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Cas No.: 10122-45-9
Sample solution is provided at 25 µL, 10mM.
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ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity[1][2].
ZZW-115 hydrochloride (0.1-33 μM; 72 hours) is efficient in killing cancer cells, with an IC50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14)[1].ZZW-115 hydrochloride (0-100 μM; 24-72 hours) is efficient to kill these tumor cells with an IC50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells)[1].ZZW-115 hydrochloride induces pancreatic cell death by necrosis and apoptosis. ZZW-115 hydrochloride treatment induces a decrease in ATP production and induces a ROS overproduction[1].LDH release is significantly higher in ZZW-115 hydrochloride-treated cells (MiaPaCa-2, 02-063, LIPC, Foie8b, and HN14 cells) than in control cells in a concentration-dependent manner. Similarly, caspase 3/7 activity is also greater in ZZW-115 hydrochloride-treated cells. These experiments demonstrated that ZZW-115 hydrochloride exerted both pronecrotic and proapoptotic effects[1]. Cell Viability Assay[1] Cell Line: ANOR cells, MiaPaCa-2, 02-063, 01008, LIPC, 02136, HN01,01046, AOIPC, Foie8b, HN14 cells
ZZW-115 hydrochloride (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors[1].ZZW-115 hydrochloride (5 mg/kg for 30 days; immunocompetent C57BL/6 mice were orthotopically implanted with Panc02 cells) treatment shows the tumor size is almost unmeasurable in some cases[1]. Animal Model: NMRI-Foxn1nu/Foxn1nu mice (nude mice) xenografted with MiaPaCa-2 cells [1]
[1]. Santofimia-CastaÑo P, et al. Ligand-based design identifies a potent NUPR1 inhibitor exerting anticancer activity via necroptosis. J Clin Invest. 2019;129(6):2500-2513. Published 2019 Mar 28. [2]. Santofimia-CastaÑo P, et al. Targeting the Stress-Induced Protein NUPR1 to Treat Pancreatic Adenocarcinoma. Cells. 2019;8(11):1453. Published 2019 Nov 17.
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