UNC0646, G9a/GLP HMTase Inhibitor


Catalog No. size PriceQuantity
M60184-2S 2 mg solid $109
M60184-10S 10mg solid $436

Description

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. 

 

 


  

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