"目录号: HY-15313

Epigenetics-

CBB1007可渗透入细胞，是hLSD1的选择性抑制剂，IC50为5.27 μM。

Histone Demethylase

相关产品

GSK-J4-GSK2879552-SP2509-Tranylcypromine hemisulfate-ORY-1001-JIB-04-ML324-IOX1-CPI-455-Daminozide-KDM5-IN-1-CBB1007 hydrochloride-DDP-38003 dihydrochloride-KDM5A-IN-1-NCGC00244536-

生物活性

Description

CBB1007 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).

References

[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.