UNC0642, G9a/GLP HMTase Inhibitor


Catalog No. size PriceQuantity
M60185-2S 2 mg solid $129
M60185-10S 10mg solid $522

Description

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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