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4°C, sealed storage, away from moisture
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货期:1-2天
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MedChemExpress LLC
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥4240.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥1590.0 |
| 规格: | 5 mg | 产品价格: | ¥3500.0 |
| 规格: | 10 mg | 产品价格: | ¥5500.0 |
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XL-784
CAS No. : 1224964-36-6
MCE 国际站:XL-784
产品活性:XL-784 是 MMP 的一个选择性抑制剂,其对 MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13 的 IC50 值分别约为 1900,0.81,120,10.8,18,0.56 nM。
研究领域:Metabolic Enzyme/Protease
作用靶点:MMP
In Vitro: XL-784 is a highly potent, low-molecular-weight (1,122 g/mol) inhibitor of MMPs that has very limited aqueous solubility (20 μg/mL). XL-784 potently inhibits MMP-2, MMP-13, andADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro, with IC50 values in the range of 1-2 nM. XL-784 also inhibits MMP-9 (IC50 ~20 nM) activity and ADAM17 (IC50 ~70 nM) also known as TACE. However, it exhibits low potency for inhibition of MMP-1 (IC50 ~2,000 nM).
In Vivo: All mice tolerate the treatments similarly. Control mice all developed aneurysms with a mean %△AD of 158.5%±4.3%. Treatment with all doses of XL-784 and doxycycline are effective in inhibiting aortic dilatation. There is a clear dose-response relationship between XL-784 and reductions in aortic dilatation at harvest (50 mg/kg 140.4% ±3.2%; 125 mg/kg 129.3% ±5.1%; 250 mg/kg 119.2%±3.5%; all Ps<0.01 compared to control). This continues with the higher doses (375 mg/kg 88.6%±4.4%; 500 mg/kg 76.0%±3.5%). The highest 2 doses of XL-784 tested are more effective than doxycycline (112.2%±2.0%, P<0.05) in inhibiting maximal dilatation of the aorta after elastase perfusion.
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文献和实验for 30-60 minutes. 3. Heat the reaction at 65degC for 10 minutes to inactivate the kinase. G. Bacterial cell maintenance Four strains of E. coli are used in these studies: JM101 for M13 infection and isolation (4), XL1BMRF
Bax- Bcl-XL二聚体中的Bax单位,进而促进细胞死亡。在体外,发现Bcl-2家族可能还对离子通道有影响。 Annexin V检测凋亡细胞的质膜变化 细胞发生凋亡时会有一系列的形态学特征性改变,其中,质膜的改变是早期凋亡的特征之一。细胞发生凋亡时,胞膜磷脂酰丝氨酸(PS)从胞膜内侧翻转到外侧,暴露于细胞外表面。Annexin V是一个35-36kD的Ca2+依赖性的磷脂结合蛋白,它与磷脂酰丝氨酸有高度亲和力,可以与细胞外暴露的磷脂酰丝氨酸结合。Annexin V标记上FITC、PE或生物
Basic procedures for bacteria culture
G. Bacterial cell maintenance Four strains of E. coli are used in these studies: JM101 for M13 infection and isolation (4), XL1BMRF' (Stratagene) for M13 or pUC-based DNA transformation (5), and ED8767 for cosmid DNA transformation
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