半岛bd体育手机客户端 说明
一般描述
A cell-permeable, lysine-specific demethylase 1 (LSD1) active site-targeting phenethylidene-benzohydrazide that inhibits LSD1 activity (IC50= 13 nM) in a reversible and substrate non-competitive (Ki= 34 nM) manner, while inhibiting CYP3A4 only at much higher concentrations (IC50= 2.61 ?M) and displaying little or no potency towards CYP1A2/2C9/2C19/2D6. MAO-A/B, D-lactate dehydrogenase, glucose oxidase, and hERG (IC50≥8.0 ?M). Shown to enhance histone H3 Lys9 dimethylation (H3K9me2) in androgen-dependent prostate cancer VCaP cultures (1 to 10 ?M) and effectively inhibits LSD1-dependent cancer growth (IC50in nM = 329/SK-N-MC, 356/AN3 Ca, 429/HT29, 468/MIA PaCa-2, 489/BT-20, 612/HER218, 614/HCT 116, 637/MCF-7, 649/T-47D; 96 h).
A cell-permeable phenethylidene-benzohydrazide compound that acts as a potent, selective, reversible, and non-competitive inhibitor of Lysine-Specific Demethylase 1 (LSD1; IC50= 13 nM; Ki= 31 nM). Exhibits excellent selectivity over monoamine oxidases A and B (IC50>300 ?M), lactate dehydrogenase, glucose oxidase, hERG, CYP1A2, CYP2D6 (IC50≥ 10 ?M), CYP2C9 (IC50= 8.04 ?M) and CYP2C19 (IC50= 9.76 ?M). Inhibits CYP3A4 only at >200-fold higher concentration. Reduces the proliferation of several cancer cell lines, including AN3 Ca, BT-20, MCF-7, T-47D, HT29, MIA PaCa-2 and SK-N-MC (IC50= 356, 489, 637, 649, 429, 468 and 329 nM, respectively).
生化/生理作用
Cell permeable: yes
Reversible: yes
Primary Target
LSD1
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
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
Fiskus, W., et al. 2014.Leukemia28,2155.
Sorna, V., et al. 2013.J. Med. Chem.56,9496.
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 | C19H20ClN3O5S |
分子量 | 437.90 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | off-white |
溶解性 | DMSO: 100 mg/mL |
储存温度 | 2-8℃ |
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