CBB1007 trihydrochloride |
رقم الكتالوجGC35624 |
CBB1007 ثلاثي هيدروكلوريد هو مركب ميدينو-جوانيدينيوم نافذ للخلايا يعمل كمثبط انتقائي LSD1 قوي وقابل للعكس وتنافسي للركيزة (IC50 = 5.27 ميكرومتر لـ hLSD1)
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Cas No.: 2070015-03-9
Sample solution is provided at 25 µL, 10mM.
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).IC50 Value: 5.27 uMTarget: hLSD1CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).
[1]. Wang J, et al. Novel histone demethylase LSD1 inhibitors selectively target cancer cells with pluripotent stem cell properties. Cancer Res. 2011 Dec 1;71(23):7238-49.
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