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产品描述： AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding |
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靶点：
IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p);HistoneMethyltransferase |
体内研究：
AMI-1 (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo. AMI-1 (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model. AMI-1 (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model |
参考文献：
1. Zhang, B., et al. Targeting protein arginine methyltransferase 5 inhibits colorectal cancer growth by decreasing arginine methylation of eIF4E and FGFR3. Oncotarget. 2015 Sep 8;6(26):22799-811. 2. Baolai Zhang, et al. Arginine Methyltransferase inhibitor-1 Inhibits Sarcoma Viability in vitro and in vivo. Oncol Lett. 2018 Aug;16(2):2161-2166. 3. Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9. |
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溶解性：
H2O : 62.5 mg/mL (113.96 mM; ultrasonic and warming and heat to 60°C) |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
1.823 ml |
9.117 ml |
18.233 ml |
| 5 mM |
0.365 ml |
1.823 ml |
3.647 ml |
| 10 mM |
0.182 ml |
0.912 ml |
1.823 ml |
| 50 mM |
0.036 ml |
0.182 ml |
0.365 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京