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| 中文名称 |
AMI-1 free acid
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|---|---|
| 中文别名 |
猩红酸;双J酸;6,6'-(1,3-亚脲基)双(1,1'-萘酚)-3,3'-磺酸;7,7-(羰基二亚氨基)二(4-羟基-2-萘磺酸);腥红酸;苯甲腈,2-氨基-5-碘;5,5'-二羟基-7,7-二磺酸基-2,2'-二萘基脲
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| 英文名称 |
AMI-1 free acid
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| 英文别名 |
7,7'-(Carbonylbis(azanediyl))bis(4-hydroxynaphthalene-2-sulfonic acid);Carbonyl J Acid;7,7-(carbonyldiimino)bis[4-hydroxy-2-naphthalenesulfonic acid];5,5-DIHYDROXY-7,7-DISULPHO-2,2-DINAPHTHYL UREA;J Acid Urea;Bis-J Acid;4,4'-dihydroxy-7,7'-ureylenedi(naphthalene-2-sulphonic acid);7,7'-(Carbonyldiimino)bis[4-hydroxy-2-naphthalenesulfonic acid];6,6'-ureylene-bis(1-naphthol-3-sulfonic acid);phosgenated;N,N'-bis(4-hydroxy-2-sulfonaphthalene-7-yl)urea;7,7'-Ureylenebis(4-hydroxy-2-naphthalenesulfonic acid);N,N'-Bis[6-(1-naphthol-3-sulfonic acid)]urea;2-Naphthalenesulfonic acid, 7,7-(carbonyldiimino)bis4-hydroxy-;J ACID UREA, FREE ACID;6,6'-ureylenbis-1-naphthol-3-sulfonic acid;66UREYLENEBIS1NAPHTHOL3SULPHONICACIDDISODIUMSALT;7,7'-(carbonyldiimino)bis[4-hydroxy-2-naphthalenesulfonic aci;Urea J Acid;Scarlet Acid;I Acid Urea;2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis[4-hydroxy-;6,6'-Ureylenebis(1-naphthol-3-sulfonic acid);NSC45174;AMI 1;4-hydroxy-7-{[(5-hydroxy-7-sulfonaph;AMI-1 free acid
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| Cas No. |
134-47-4
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| 分子式 |
C21H16N2O9S2
|
| 分子量 |
504.49
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| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
AMI-1 free acid 是一种有效的，细胞渗透性的，可逆的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂，对人 PRMT1 和酵母 Hmt1p 作用的 IC50 值分别为 8.8 μM 和 3.0 μM。AMI-1 free acid 通过阻断肽-底物结合对 PRMTs 发挥抑制作用。
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| 生物活性 |
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC 50 s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)
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| 体外研究(In Vitro) |
AMI-1 free acid can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p).AMI-1 free acid not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5. AMI-1 free acid specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site. AMI-1 free acid inhibits methylation of GFP-Npl3 and cellular proteins.AMI-1 free acid (0.6-2.4 mM; 48-96 hours) inhibits the cell viability of sarcoma in S180 and U2OS cells in a time-dependent and dose-dependent manner in vitro.AMI-1 free acid (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis. has not independently confirmed the accuracy of these methods.
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| 体内研究(In Vivo) |
AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo.
AMI-1 free acid (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 free acid (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| 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.
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| 溶解度数据 |
In Vitro: DMSO : 83.33 mg/mL (165.18 mM; Need ultrasonic)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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