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AMI-1

PRMT1抑制剂,Potent, cell permeable and specific protein arginine N-methyltransferase 1 (PRMT1) inhibitor (IC50 = 8, 8 µM), Does not compete for the AdoMet (S-adenosyl-L-methionine, SAM) binding site, Blocks peptide substrate binding, HIV-1 RT polymerase inhi

目录号: PC10026 纯度: ≥98%

CAS No. :20324-87-2

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PC10026-5mg	5mg	¥686.00	请登录
PC10026-25mg	25mg	¥2058.00	请登录

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中文名称	AMI-1
中文别名	猩红酸钠盐;6,6'-(1,3-亚脲基)双(1-萘酚-3-磺酸钠);猩红酸钠
英文名称	AMI-1
英文别名	Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate);7,7'-(Carbonyldiimino)bis(4-hydroxy-2-naphthalenesulfonic acid) disodium salt;AMI-1;SODIUM 6,6'-(1,3-UREYLENE)BIS(1-NAPHTHOL-3-SULFONATE);disodium 4-hydroxy-7-[(5-hydroxy-7-sulfonato-2-naphthyl)carbamoylamino]naphthalene-2-sulfonate;Disodium 6,6'-ureylenebis[1-naphthol-3-sulfonate];SODIUM 6,6'-(1,3-UREYLENE) BIS(1,1'-NAPHTHOL)-3,3'-SULFONATE;2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis[4-hydroxy-, sodium salt (1:2);AMI 1;2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis(4-hydroxy-, sodium salt (1:2);disodium;4-hydroxy-7-[(5-hydroxy-7-sulfonatonaphthalen-2-yl)carbamoylamino]naphthalene-2-sulfonate;7,7'-(Carbonyldiimino)bis[4-hydroxy-2-n
Cas No.	20324-87-2
分子式	C₂₁N₂O₉Na₂S₂H₁₄
分子量	548.45
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

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.

性状

Solid

IC50 & Target[1][2]

IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p)

体外研究(In Vitro)

AMI-1 can inhibit the 体外研究 methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p).
AMI-1 not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5.
AMI-1 specifically inhibits arginine, but not lysine, methyltransferase activity 体外研究 and does not compete for the AdoMet binding site.
AMI-1 inhibits methylation of GFP-Npl3 and cellular proteins.
AMI-1 (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 体外研究.
AMI-1 (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	S180 cells, U2OS cells
Concentration:	0.6 mM, 1.2 mM, 2.4 mM
Incubation Time:	48 hours, 72 hours, 96 hours
Result:	Inhibited the cell viability.

Apoptosis Analysis

Cell Line:	S180 cells
Concentration:	1.2 mM, 2.4 mM
Incubation Time:	48 hours, 72 hours
Result:	Increased the percentages of cells undergoing apoptosis.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft
Dosage:	0.5 mg
Administration:	Intratumorally, daily, for 7 days
Result:	Decreased tumor weight.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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. [Information]

[2]. Baolai Zhang, et al. Arginine Methyltransferase inhibitor-1 Inhibits Sarcoma Viability 体外研究 and in vivo. Oncol Lett. 2018 Aug;16(2):2161-2166. [Information]

[3]. Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9. [Information]

溶解度数据

体外研究:

H₂O : 62.5 mg/mL (113.96 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8233 mL	9.1166 mL	18.2332 mL
5 mM	0.3647 mL	1.8233 mL	3.6466 mL
10 mM	0.1823 mL	0.9117 mL	1.8233 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (182.33 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

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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