LCH-7749944

SKU: orb1219723

Description

LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis. LCH-7749944 is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase. LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner. LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner. LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells.

Key Properties

• CAS Number: 796888-12-5
• MW: 350.41
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂N₄O₂
• SMILES: COc1cccc(Nc2nc(NCC3CCCO3)c3ccccc3n2)c1
• Target: Apoptosis
• Solubility: DMSO:250 mg/mL (713.45 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  Cell Proliferation Assay Cell line: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells. Concentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM. Incubation time: 24 hours. Result: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner. Apoptosis Analysis Cell line: SGC7901 cells. Concentration: 5, 10, 20 μM. Incubation time: 12, 24, 48 hours. Result: Induced apoptosis of SGC7901 cells. Cell Cycle Analysis Cell line: SGC7901 cells. Concentration: 5, 10, 20 μM. Incubation time: 12, 24, 48 hours. Result: Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase. Western blot analysis. Cell line: SGC7901 cells. Concentration: 5, 10, 20, 30 μM. Incubation time: 24 hours. Result: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.

Storage & Handling

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

Alternative Names

GNF-PF-2356

Quick Database Links

Gene Symbol

Apoptosis