产品说明
一般描述
A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 µM for hLSD1) and efficiently blocks 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). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 >100 µM).
A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 µM for hLSD1) and efficiently blocks 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). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 >100 µM).
Note: the molecular weight is lot-specific and can be found on the vial label.
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
外形
Supplied as a trifluoroacetate salt.
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Wang, J., et al. 2011. Cancer Res.71, 7238.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C27H34N8O4 · 3C2HF3O2 |
分子量 | 876.68 |
MDL编号 | MFCD25976706 |
产品性质
质量水平 | 100 |
测定 | ≥99% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
颜色 | white |
溶解性 | DMSO: 50 mg/mL |
运输 | ambient |
储存温度 | −20℃ |
SMILES string | NC(N1CCN(CC2=CC(C(N3CCN(C(C4=CC=C(C(N)=N)C=C4)=O)CC3)=O)=CC(C(OC)=O)=C2)CC1)=N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich