Matrix metalloproteinases (MMPs) play important roles in tumor invasion, metastasis, and angiogenesis. Batimastat is a synthetic, low molecular weight, hydroxamate-based inhibitor of MMPs. It inhibited MMP-1, 2, 3, 9, 13, and 14 with IC50 values of 0.99, 0.73, 0.56, 0.60, 5.0, and 4.6 nM, respectively. It also blocked the activity of TNF-α converting enzyme with an IC50 value of 14.9 nM[3]. Batimastat showed less inhibitory effect on the processing of CD23, a low affinity IgE receptor, with an IC50 value of 100 nM[4]. In athymic mice inoculated with MDA435/LCC6 human breast cancer cells, daily injection of 50 mg/kg batimastat for 28 days significantly reduced tumor volumes relative to vehicle-treated controls[5].
作用机制
Batimastat inhibits the activity of MMPs via binding the zinc ion in the catalytic site of MMPs.
Batimastat 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
Sf9 insect cells
Function assay
Inhibition of human matrix metalloprotease-2 expressed in Sf9 insect cells, IC50=0.013 μM
15582436
Sf9 insect cells
Function assay
Inhibition of human matrix metalloprotease-9 expressed in Sf9 insect cells, IC50=0.025 μM
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