UNC-0642 Inhibitor

POWDER

99.5%

For 3 years at -20 degree C (powder)
For 2 years -80 degree C in solvent.

546.69

1481677-78-4

C29H44F2N6O2

Chromatin/Epigenetic

CC(N1CCC(Nc2c3cc(OC)c(OCCCN4CCCC4)cc3nc(N3CCC(F)(F)CC3)n2)CC1)C

G9a/GLP

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.1,2,3 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. 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. Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734). See the Structural Genomics Consortium (SGC) website for more information.

For obtaining a higher solubility, please warm the tube at 37 degree C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 degree C for several month.