ZZW-115是一种有效的NUPR1抑制剂，Kd为2.1μM，通过坏死和凋亡(apoptosis)诱导肿瘤细胞死亡。具有抗癌活性。
货号:ajcx31686
CAS:801991-87-7
分子式:C24H31F3N4S
分子量：464.59
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity[1][2].

ZZW-115 (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 (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 induces pancreatic cell death by necrosis and apoptosis. ZZW-115 treatment induces a decrease in ATP production and induces a ROS overproduction[1].LDH release is significantly higher in ZZW-115-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-treated cells. These experiments demonstrated that ZZW-115 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 (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors[1].ZZW-115 (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.