| 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. |
| 体外研究： |
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 |
| 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 |
| 参考文献： |
1. Bachovchin DA, et al. Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J Med Chem. 2011 Jul 28;54(14):5229-36. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.167 ml |
10.836 ml |
21.671 ml |
| 5 mM |
0.433 ml |
2.167 ml |
4.334 ml |
| 10 mM |
0.217 ml |
1.084 ml |
2.167 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.433 ml |
|
| 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。 |
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