Prinomastat普啉司他,192329-42-3

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Prinomastat

CAS No. : 192329-42-3

MCE 国际站：Prinomastat

产品活性：Prinomastat (AG3340) 是一种广谱，有效的口服活性金属蛋白酶 (MMP) 抑制剂，对于 MMP-1, MMP-3 和 MMP-9 的 IC₅₀ 分别为 79 nM，6.3 nM 和 5.0 nM。Prinomastat 抑制 MMP-2, MMP-3 和 MMP-9 的 K_i 分别为 0.05 nM，0.3 nM 和 0.26 nM。Prinomastat 穿过血脑屏障。抗肿瘤活性。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：MMP  |  Apoptosis

In Vitro: Prinomastat (AG3340; 0.1-1 µg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat.
Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat (AG3340).
Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. As anticipated, the migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells.The effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat in C57MG/Wnt1 cells.

In Vivo: In a human fibrosarcoma mouse model (HT1080), the mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumour inoculation. Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition, with a short T_1/2 of 1.6 hours.

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