JK-P3

SKU: orb1222979

Description

JK-P3 is novel inhibitor of VEGFR-2. JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50 = 7.8 μM). JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endothelial cell proliferation.

Key Properties

• CAS Number: 942655-44-9
• MW: 323.35
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₇N₃O₃
• SMILES: COc1c(cc(cc1)C(=O)Nc1n[nH]c(c1)c1ccccc1)OC
• Target: VEGFR2
• Solubility: In Vitro: DMSO : 50 mg/mL (154.63 mM)

Bioactivity

• In Vitro:
  JK-P3 (0.01-10 μM; 1 hour) inhibits VEGF-A-mediated VEGFR2 phosphorylation and downstream signalling. JK-P3 (0.01-10 μM; 16 hours) dose not inhibit HUVEC cell proliferation at 0.01~1 μM, and shows slight inhibitory activity at 10 μM. JK-P3 (1 and 10 μM; 1 hour) does not significantly inhibit VEGF-A-stimulated endothelial tube formation at 1 μM, but almost completely inhibits the ability of endothelial cells to form into elongated hollow tubes in the presence of VEGF-A at 10 μM. Western blot analysis. Cell line: Primary endothelial cells (treated for 7.5 min with 25 ng/mL VEGF-A) Concentration: 0.01, 0.1, 1 and 10 μM Incubation time: 1 hour. Result: Almost completely inhibited VEGFR2 Y1175 phosphorylation, also inhibited VEGF-A-stimulated PLCγ1, Akt and ERK1/2 phosphorylation. Cell Proliferation Assay Cell line: HUVEC. Concentration: 0.01, 0.1, 1 and 10 μM Incubation time: 16 hours. Result: Failed to inhibit endothelial cell proliferation at 0.01~1 μM but elicited a small but significant increase in cell proliferation at certain lower concentrations.

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

3,4-Dimethoxy-N-(5-phenyl-1H-pyrazol-3-yl)-benzamide

Quick Database Links

Gene Symbol

VEGFR2