| 产品描述： | UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM |
| 靶点： |
G9a:4 nM (IC50);HistoneMethyltransferase |
| 体外研究： |
UNC 0631 (化合物 7) 在多种细胞系中具有高细胞效力和功能效力与细胞毒性的出色分离。UNC 0631 在降低 H3K9me2 水平方面非常有效并且具有低细胞毒性。UNC 0631在 MDA-MB-231、MCF7、PC3、22RV1、HCT116 wt、HCT116 p53-/-和IMR90细胞系中分别以25 nM、18 nM、26 nM、24 nM、51 nM、72 nM和46 nM的ICW IC50值降低H3K9me2水平 |
| 细胞实验： |
MDA-MB-231, PC3, HCT116 cells are cultured in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Cells are treated with inhibitors for 48 h. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1mg/mL of MTT and incubated for 1–2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazanis solubilized in acidified isopropanol and 1% Triton. Formazan signal absorbance is measured at 570 nm and corrected for the 650 nm background. IC50s are calculated using GraphPad Prizm statistical package with sigmoidal variable slope dose response curve fit.(Only for Reference) Cell lines: MDA-MB-231, PC3, HCT116, 22RV1, MCF7 and IMR90 cells |
| 参考文献： |
1. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. |
| 溶解性： |
Soluble in DMSO、Ethanol、DMF |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.573 ml |
7.863 ml |
15.725 ml |
| 5 mM |
0.315 ml |
1.573 ml |
3.145 ml |
| 10 mM |
0.157 ml |
0.786 ml |
1.573 ml |
| 50 mM |
0.031 ml |
0.157 ml |
0.315 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京