PNC-27 CAS:1159861-00-3

Name:  Lynn
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Email：    guangsheng 5   @zgguangsheng.com

I. Core Structure & Properties

II. Mechanism of Action

1. Membrane HDM-2 Binding: Binds to HDM-2 overexpressed on cancer cell membranes (minimal on normal cells).
2. Pore Assembly: HDM-2-PNC-27 complexes oligomerize into transmembrane pores, disrupting membrane integrity.
3. Mitochondrial Damage: Cytosolic PNC-27 forms pores in mitochondrial membranes, amplifying cell death.
4. Necrotic Cell Death: Rapid lysis occurs within 4 hours via necrosis, independent of p53 function.

III. Preclinical Efficacy & Applications

• Broad Antitumor Activity: Active against breast, colon, lung, ovarian, cervical, melanoma, osteosarcoma, and leukemia (including p53-null/K562 cells) in vitro/in vivo.
• Resistance Overcoming: Effective against chemotherapy-resistant lines (e.g., paclitaxel-resistant ovarian cancer).
• Research Uses:
  • Probe HDM-2 membrane biology and cancer-specific membrane vulnerabilities.
  • Develop targeted delivery systems (nanoparticles) for imaging and therapy.
  • Validate MRP-based peptide design for cell penetration and membrane targeting.
  
  

IV. Research Protocols & Safety

1. Handling & Reconstitution: Use PPE; reconstitute with sterile water/saline; discard unused solution after 24–48 hours.
2. Typical Dosing: In vitro: 5–20 μM (24–72 h incubation); in vivo: 1–5 mg/kg (intravenous/intratumoral, 2–3× weekly).
3. Safety Notes: Minimal normal cell toxicity; potential local irritation at injection sites. Dispose of waste per laboratory safety guidelines.