AMI-1 free acid
目录号 : KM18967 CAS No. : 134-47-4 纯度 : ≥98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg 询价 In-stock
100mg 询价 In-stock

Other Forms of Rapamycin:

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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 IC50s 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.

体外研究

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.

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

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.

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.
分子式
C21H16N2O9S2
分子量
504.49
CAS号
134-47-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (165.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9822 mL 9.9110 mL 19.8220 mL
5 mM 0.3964 mL 1.9822 mL 3.9644 mL
10 mM 0.1982 mL 0.9911 mL 1.9822 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.12 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.12 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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