JK-P3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JK-P3 是一种基于吡唑的 VEGFR-2 抑制剂（IC50：7.8 μM）。 JK-P3 在体外抑制 FGFR 1/3 激酶活性，但在细胞检测中对 FGFR 信号传导没有影响。

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.

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.

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

Others

Other Targets

VEGFR2

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942655-44-9

323.35

C18H17N3O3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (154.63 mM)

COc1c(cc(cc1)C(=O)Nc1n[nH]c(c1)c1ccccc1)OC

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

(-20℃)

With Ice Pack

≥ 2 years