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| 描述 | ZZW-115 is a potent NUPR1 inhibitor with a Kd value of 2.1 μM. ZZW-115 induces tumour cell death through necrosis and apoptosis[1][2].ZZW-115 was effective in killing cancer cells in the concentration range of 0.1-33 μM for 72 h. The IC50 of ZZW-115 ranged from 0.84 μM (ANOR) to 4.93 μM (HN14). ZZW-115 induced necrosis and apoptosis of pancreatic cells, and during its action, it caused a decrease in the production of ATP and induced the overproduction of ROS. LDH release from ZZW-115-treated cells (MiaPaCa-2, 02-063, LIPC, Foie8b and HN14 cells) was significantly higher than that from control cells in a concentration-dependent manner. Similarly, caspase 3/7 activity was higher in ZZW-115-treated cells. These experiments suggest that ZZW-115 also has a pro-apoptotic effect[1]. |
| Concentration | Treated Time | Description | References | |
| MiaPaCa-2 cells | 6 µM | 6 hours | Inhibition of NUPR1 activity impeded SGs formation | EMBO Mol Med. 2024 Mar;16(3):475-505 |
| MiaPaCa-2 cells | 6 µM | 6 hours | Inhibition of NUPR1 activity impeded SGs formation | J Clin Invest. 2019 Mar 28;129(6):2500-2513. |
| U87 and U251 glioblastoma cells | 1.5 µM | 12 hours | To evaluate the enhancing effect of ZZW-115 on DNA damage induced by genotoxic agents (e.g., TMZ) in glioblastoma cells. | JCI Insight. 2020 Sep 17;5(18):e138117 |
| AOIPC primary PDAC cells | 1.5 µM | 12 hours | To evaluate the enhancing effect of ZZW-115 on DNA damage induced by different genotoxic agents (5-FU, oxaliplatin, γ-radiation, and gemcitabine) in PDAC cells. | JCI Insight. 2020 Sep 17;5(18):e138117 |
| MiaPaCa-2 cells | 3 or 5 µM | 24 hours | Demonstrated that our compound was able to induce cell death by apoptosis and necroptosis on a dose-dependent manner, by measuring caspase 3/7 activity or LDH release, respectively. | Cells. 2019 Nov 17;8(11):1453 |
| HCC cells (Huh7, PLC/PRF/5, Hep3B, LM3, MHCC-97H, MHCC-97L, SNU449, SNU387, HepG2) | 5 µM | 24 hours | ZZW-115 inhibits NUPR1 activity, increases intracellular Fe2+ and lipid ROS levels, decreases GSH levels, induces ferroptosis, and thereby inhibits the proliferation and migration of HCC cells. | Mol Cancer. 2024 May 28;23(1):113 |
| Pancreatic cancer cells | 1 µM | 24 hours | The cell death effect induced by ZZW-115 was systematically inhibited by olaparib, whereas PDD00017273 treatment enhanced the cell death effect. | Commun Biol. 2022 Jul 22;5(1):732. |
| MiaPaCa-2 cells | 1.5 µM | 24 hours | ZZW-115 treatment induced a strong increase in PARylation which is almost completely rescued by Ferrostatin-1, NAC, and Mitoquinone treatments. | Commun Biol. 2022 Jul 22;5(1):732. |
| DLD1 cells | 1 µM | 24 hours | ZZW-115 significantly increased the level of lipid peroxidation in RR cells and restored the sensitivity of RR cells to radiotherapy. | J Cell Mol Med. 2025 Apr;29(7):e70519 |
| RKO cells | 1 µM | 24 hours | ZZW-115 significantly increased the level of lipid peroxidation in RR cells and restored the sensitivity of RR cells to radiotherapy. | J Cell Mol Med. 2025 Apr;29(7):e70519 |
| HepG2 cells | 0.5-1.4 µM | 24-72 hours | To evaluate the effect of ZZW-115 on cell survival, results showed that Fer-1 (1 µM) increased cell viability and reduced intracellular ROS production. | Cell Death Discov. 2021 Oct 1;7(1):269 |
| MiaPaCa-2 cells | 0.5-1.4 µM | 24-72 hours | To evaluate the effect of ZZW-115 on cell survival, results showed that Fer-1 (1 µM) increased cell viability and reduced intracellular ROS production. | Cell Death Discov. 2021 Oct 1;7(1):269 |
| 9805 i-Kras cells | 6 µM | 6 hours | Induced cell death in cells with activated KrasG12D, activated caspase 3 and released LDH | J Clin Invest. 2019 Mar 28;129(6):2500-2513. |
| 9805 i-Kras cells | 6 µM | 6 hours | Induced cell death in cells with activated KrasG12D, activated caspase 3 and released LDH | EMBO Mol Med. 2024 Mar;16(3):475-505 |
| MiaPaCa-2 cells | 5 µM | 6 hours | To study the effect of ZZW-115 on NUPR1 nuclear translocation, results showed that ZZW-115 almost completely inhibited the translocation of NUPR1 from the cytoplasm to the nucleus. | JCI Insight. 2020 Sep 17;5(18):e138117 |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c nude mice | HCC xenograft model | Intraperitoneal injection | 5 mg/kg | Every five days for 25 days | The combination of ZZW-115 and lenvatinib significantly inhibited the growth of HCC xenografts and enhanced the sensitivity of HCC cells to lenvatinib by inducing ferroptosis. | Mol Cancer. 2024 May 28;23(1):113 |
| Nude mice | PANC1 or MIAPaCa2 xenograft models | Intraperitoneal injection | 5 mg/kg | Once every other day for 2 weeks | ZZW-115 increased the anticancer activity of IKE | Nat Commun. 2021 Jan 28;12(1):647. |
| Animal study | Immunocompetent C57BL/6 mice were orthotopically implanted with Panc02 cells. ZZW-115 inhibited the growth of pancreatic xenograft tumours in mice at a dose of 0.5-5 mg/kg administered by daily injection for 30 days[1]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.22mL |
10.76mL 2.15mL 1.08mL |
21.52mL 4.30mL 2.15mL |
|
| CAS号 | 801991-87-7 |
| 分子式 | C24H31F3N4S |
| 分子量 | 464.59 |
| SMILES Code | FC(F)(F)C1=CC=C(SC2=C3C=CC=C2)C(N3CCCN4CCN(CC4)CCN(C)C)=C1 |
| MDL No. | MFCD34469422 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
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