产品详情
简单介绍：
UNC0642,G9a/GLPHMTaseInhibitor
详情介绍：
Product Information
| Molecular Weight: | 546.70 |
| Formula: | C29H44F2N6O2 |
| Purity: | ≥98% |
| CAS#: | 1481677-78-4 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 2-(4,4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
UNC0642 is a novel highly potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC50 < 2.5 nM. It has selectivity > 1000-fold over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50~110 nM). It has improved PK properties relative to UNC0638 and displayed modest brain penetration in vivo.
How to Use:
- In vitro: UNC0642 was used at 0.5 µM in vitro and cellular assays.
- In vivo: UNC0642 was dosed to mice by intraperitoneal injection (IP) at 5 mg/kg once per day.
Reference:
- 1. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. (2013) J Med Chem. 56(21):8931-42.
Products are for research use only. Not for human use.
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