普马司他
| 中文名称 | 普马司他 |
|---|---|
| 中文同义词 | 普马司他;(S)-2-[(羟基氨基)甲基]-5,6-二甲基-4-(4-吡啶-4-基氧苯基)磺酰基吗啉-3-硫酮;MMP抑制剂(PRINOMASTAT);普啉司他;化合物 T12539L |
| 英文名称 | Prinomastat |
| 英文同义词 | (S)-2,2-DIMETHYL-N-HYDROXY-4-[4-(4-PYRIDYLOXY)PHENYLSULFONYL]-1,4-THIAZINANE-3-CARBOXAMIDE;3-Thiomorpholinecarboxamide, N-hydroxy-2,2-dimethyl-4-((4-(4-pyridinyloxy)phenyl)sulfonyl)-, (S)-;Ag 3340;Ag3340;Ag-3340;KB-R 9896;(S)-2,2-Dimethyl-4-((p-(4-pyridyloxy)phenyl)sulfonyl)-3-thiomorpholinecarbohydroxamic acid hydrochloride;AG 3340 hydrochloride |
| CAS号 | 192329-42-3 |
| 分子式 | C18H21N3O5S2 |
| 分子量 | 423.51 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 192329-42-3.mol |
| 结构式 |  |
普马司他 性质
| 熔点 | 149.8° |
|---|---|
| 密度 | 1.377±0.06 g/cm3(Predicted) |
| 储存条件 | room temp |
| 溶解度 | 在水中的溶解度为15mg/mL（澄清溶液） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.25±0.23(Predicted) |
| 颜色 | 白色至米色 |
|
MMP-9 5 nM (IC 50 ) |
MMP-9 0.26 nM (Ki) |
MMP-2 0.05 nM (Ki) |
MMP-1 79 nM (IC 50 ) |
MMP-3 6..3 nM (IC 50 ) |
MMP-3 0.3 nM (Ki) |
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.
Western Blot Analysis
| Cell Line: | C57MG/Wnt1 cells |
| Concentration: | 0.1 µg/mL, 1 µg/mL |
| Incubation Time: | 4 days |
| Result: | A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells. |
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.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12170 | 普马司他 Prinomastat | 192329-42-3 | 1mg | 1250元 |
| 2024/04/30 | HY-12170 | 普马司他 Prinomastat | 192329-42-3 | 5mg | 3750元 |