产品详情
简单介绍：
UNC0646,G9a/GLPHMTaseInhibitor
详情介绍：
Product Information
| Molecular Weight: | 621.90 |
| Formula: | C36H59N7O2 |
| Purity: | ≥98% |
| CAS#: | 1320288-17-2 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | N-(1-cyclohexylpiperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
UNC0646 is a novel potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC50 ~6 nM and 15 nM for G9a and GLP, respectively. It potently inhibits G9a/GLP methyltransferase activity in cells (IC50 ~10 nM in MCF7 cells), and exhibits low toxicity. It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases. UNC0646 did not affect G9a co-activator function but selectively decreased G9a co-repressor function for endogenous target genes.
How to Use:
- In vitro: UNC0646 was used at 2 µM in vitro and cellular assays.
- In vivo: n/a
Reference:
- 1. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. (2011) J Med Chem. 54(17):6139-50.
- 2. Bittencourt D, et al. G9a functions as a molecular scaffold for assembly of transcriptional coactivators on a subset of glucocorticoid receptor target genes. (2012) Proc Natl Acad Sci USA. 109(48):19673-8.
Products are for research use only. Not for human use.
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