ZZW-115

SKU: orb2900262

Description

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.

Key Properties

• CAS Number: 801991-87-7
• MW: 464.59
• Purity: >98% (HPLC)
• Formula: C₂₄H₃₁F₃N₄S
• SMILES: C(CCN1CCN(CCN(C)C)CC1)N2C=3C(SC=4C2=CC=CC4)=CC=C(C(F)(F)F)C3

Bioactivity

• In Vivo:
  ZZW-115 (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors. 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. Animal model: NMRI-Foxn1nu/Foxn1nu mice (nude mice) xenografted with MiaPaCa-2 cells. Dosage: 5, 2.5, 1.0, or 0.5 mg/kg. Administration: Injection, daily for 30 days. Result: When the mice were injected with 5 mg/kg ZZW-115, the tumors stopped growing a few days after treatment and their size decreased progressively, almost disappearing at the end of the treatment.
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• In Vitro:
  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). 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). ZZW-115 induces pancreatic cell death by necrosis and apoptosis. ZZW-115 treatment induces a decrease in ATP production and induces a ROS overproduction. 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. Cell Viability Assay Cell line: ANOR cells, MiaPaCa-2, 02-063, 01008, LIPC, 02136, HN01, 01046, AOIPC, Foie8b, HN14 cells. Concentration: 0.1- 33 μM Incubation time: 72 hours. Result: Was efficient in killing cancer cells, with an IC50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14). Cell Proliferation Assay Cell line: U87, A375, U2OS, SaOS-2, HT29, SK-CO-1, LS174T, H1299 and H358, HepG2, PC3, THP-1, Daudi, Jurkat and MDA-MB-231 cells. Concentration: 0-100 μM. Incubation time: 24 or 72 hours. Result: Was 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).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only