LSD1 fluorometric drug discovery kit
LSD1 (lysine-specific histone demethylase 1) 為組蛋白 H3 的去甲基化酵素，可專一性移除連結於 H3 序列中第四個胺基酸 "Lysine" 的單甲基團與雙甲基團 (H3K4me1, H3K4me2)。目前已知 LSD1 的過度表現與多種癌症具有相關性，被視為是極有潛力的藥物開發標的。
Enzo Life Sciences 所開發的「LSD1 fluorometric drug discovery kit」是藉由 LSD1 去甲基化過程中會產生 H2O2 的特性，使得 CELLESTIAL® Red Peroxidase Substrate 能夠在 H2O2 存在下經由 HRP 酵素催化為螢光物質 (Ex/Em: 530-570/590 nm)*。當 LSD1 酵素活性越高時，所測得的螢光訊號也就越強。LSD1 fluorometric drug discovery kit 內含所有酵素活性分析所需試劑，讓研究者能夠快速便利地進行 LSD1 調控藥物的篩選試驗。
*除螢光訊號外，亦可測得 563 nm 吸收光。
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產品效能
Tranylcypromine Inhibition of LSD1. LSD1 enzyme (0.1 µg/µg) was incubated with the indicated concentrations of tranylcypromine for 30 min. at room temperature (23°C). Samples (0.5 µg, 5 µl) were then transferred to wells for the demethylation assay with 20 µM H3K4Me2 peptide. Fluorescence was measured at 47 sec intervals on a CytoFluor™ II fluorescence plate reader (PerSeptive Biosystems, Ex. 530 nm, Em. 590 nm, gain = 60). Initial rates were obtained from linear least squares fits to the 0-141 sec data as described in user mamual "Time Courses" section. The dose-response curve was derived from a least squares fit to the 4-parameter Hill-Slope model, y =‘bottom + (top – bottom)/(1 + (x/IC50)slope) (‘Solver’ tool, Microsoft, Excel). The fitted parameter values were: top = 3.74 AFU/sec; bottom = 0.696 AFU/sec; IC50 = 20.1 µM; slope = 1.98.
訂購資訊
| Product Name | Pack Size | Cat. No. |
|---|---|---|
| LSD1 fluorometric drug discovery kit Kit Components: Recombinant human LSD1, H3K4Me2 Peptide, HRP, CELLESTIAL® Red Peroxidase Substrate, H2O2 Standard, LSD1 Inhibitor "Tranylcypromine", 96-well Plate, etc. |
1 Kit (96 assays) | BML-AK544-0001 |
