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CBB1007 trihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CBB1007 trihydrochloride图片

CBB1007三盐酸盐是LSD1选择性抑制剂,IC50值为5.27uM。
Canonical SMILESNC(N1CCN(CC1)CC2=CC(C(OC)=O)=CC(C(N3CCN(CC3)C(C4=CC=C(C=C4)C(N)=N)=O)=O)=C2)=N.[H]Cl.[H]Cl.[H]Cl
分子式C27H37Cl3N8O4
分子量643.99
溶解度DMSO: ≥ 54 mg/mL (83.85 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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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