半岛bd体育手机客户端 说明
一般描述
A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC50= 6.4 ?M; Ki= 5.5 ?M) and KDM4B (IC50= 9.3 ?M; Ki= 3.0 ?M) and completely blocks their demethylating activity toward H3K9me3 (~ 5 ?M). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC50= 16.5 ?M after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 ?M over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC50= 6.4 ?M; Ki= 5.5 ?M) and KDM4B (IC50= 9.3 ?M; Ki= 3.0 ?M) and completely blocks their demethylating activity toward H3K9me3 (~ 5 ?M). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC50= 16.5 ?M after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 ?M over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.
生化/生理作用
Cell permeable: yes
Primary Target
KDM4A/B
Reversible: yes
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 3 months at -20°C.
其他说明
Chu, C.H., et al. 2014.Journ. Med. Chem.57,5975.
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 | C22H12Cl4N2O4 |
分子量 | 510.15 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
效能 | 3.0 μM Ki |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | brown |
溶解性 | DMSO: 10 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