Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMZ30是磷酸酯酶PME-1高效抑制剂(IC50:600nM)。它可减少活细胞中 PP2A 的去甲基化形式。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
5 mg | ¥ 618 | 现货 | ||
10 mg | ¥ 990 | 现货 | ||
25 mg | ¥ 1,670 | 现货 | ||
50 mg | ¥ 2,490 | 现货 | ||
100 mg | ¥ 3,670 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,090 | 现货 |
产品描述 | AMZ30 is a selective inhibitor of PME-1 (IC50: 600 nM). It also reduces the demethylated form of PP2A in living cells. |
靶点活性 | PME-1:600 nM |
体外活性 | Incubation of HEK 293T cells with a concentration range of AMZ30 generated an in situ IC50 value for PME-1 inhibition of 3.5 μM. In HEK 293T cells stably overexpressing PME-1, AMZ30 (20 μM) caused an ~80% reduction in the levels of demethylated PP2A. AMZ30 treatment also significantly increased the methylated form of PP2A. AMZ30 (20 μM) also decreased the demethylated form of PP2A to a similar degree in untransfected HEK 293T cells expressing basal levels of PME-1. |
激酶实验 | Purified wild-type PME-1 (500 nM, 2.6 mL total volume in PBS) was incubated with DMSO or AMZ30 (50 μM) at 25 °C. After 30 min, 100 μL was removed from each reaction (Fraction A). The remaining 2.5 mL of each reaction was passaged over a Sephadex G-25M column and eluted in a volume of 3.5 mL PBS (Fraction B). 100 μL of both fractions A and B were labeled with FP-rhodamine (2 μM). After 30 min, the reactions were quenched with 2× SDS-PAGE loading buffer, separated by SDS-PAGE, and analyzed by in-gel fluorescence scanning. Gels were then subjected to Coomassie staining with InstantBlue to verify equivalent protein loading. |
细胞实验 | HEK 293T cells were grown in DMEM SILAC media supplemented with dialyzed fetal bovine serum and 12C14N-lysine and - arginine for "light" cells or 13C615N2-lysine and -arginine for "heavy" cells. Cells were treated as indicated with DMSO or 28 (1 h, 37 °C), washed, harvested, and soluble and membrane proteomes were isolated as described above. Light and heavy proteome fractions (0.5 mg each) were combined (1 mL total volume) and labeled with 5 μM of FP-biotin for 1 hr at 25 °C. After incubation, the membrane proteomes were solubilized with 1% Triton-X and rotated at 4 °C for 1 hr. Enrichment of FP-labeled proteins was achieved as previously described.34 The streptavidin-enriched proteome was washed two times for 3 min with (1) 1% SDS in PBS, (2) 6 M urea in PBS, (3) PBS (pH 7.5) and finally resuspended in 200 μL 8 M urea in 25 mM ammonium bicarbonate. Samples were then prepared for on-bead digestion by reduction with 10 mM TCEP for 30 min at 25 °C and alkylation with 12 mM iodoacetamide for 30 min at 25 °C in the dark. Samples were diluted to 2 M urea with PBS (pH 7.5) and digestions were performed for 12 hr at 37 °C with sequence-grade modified trypsin (4 μL of 0.5 μg/μL) in the presence of 2 mM CaCl2. Lastly, peptide samples were acidified with formic acid to a final concentration of 5%. |
分子量 | 461.44 |
分子式 | C19H12FN3O6S2 |
CAS No. | 1313613-09-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (48.76 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1671 mL | 10.8356 mL | 21.6713 mL | 54.1782 mL |
5 mM | 0.4334 mL | 2.1671 mL | 4.3343 mL | 10.8356 mL | |
10 mM | 0.2167 mL | 1.0836 mL | 2.1671 mL | 5.4178 mL | |
20 mM | 0.1084 mL | 0.5418 mL | 1.0836 mL | 2.7089 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AMZ30 1313613-09-0 Others AMZ-30 inhibit Inhibitor AMZ 30 inhibitor