A selective inhibitor of G9a and GLP methyltransferases that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM; reduces H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells (IC50s = 110 and 40 nM

UNC0642 – 5 mg

Brand:
Cayman
CAS:
1481677-78-4
Storage:
-20
UN-No:
Non-Hazardous - /

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.{28474} UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.{28474} Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).{28474} See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A selective inhibitor of G9a and GLP methyltransferases that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM; reduces H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells (IC50s = 110 and 40 nM, respectively); displays improved pharmacokinetic properties relative to UNC0638

Formal name: 2-(4,4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine

Synonyms: 

Molecular weight: 546.7

CAS: 1481677-78-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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