UNC0646,G9a/GLPHMTaseInhibitor
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產品名稱: UNC0646,G9a/GLPHMTaseInhibitor
產品型號: M60184-2s
產品展商: 其它品牌
產品文檔: 無相關文檔
簡單介紹
UNC0646,G9a/GLPHMTaseInhibitor
UNC0646,G9a/GLPHMTaseInhibitor
的詳細介紹
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.?
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How to Use:
- In vitro:? UNC0646 was used at 2 μM in vitro and cellular assays.?
- In vivo:?n/a
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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.?
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Products are for research use only. Not for human use.
