BIX 01294

Short Summary : G9a and GLP inhibitor

Category : Chromatin/Epigenetics|Histone Methyltransferase

Purity : 0.98

CAS Number : 935693-62-2

Formula : C28H38N6O2

Molecular Weight : 490.65

SMILE : CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC

Solubility : >24.45mg/mL in DMSO

Storage : Store at -20°C

Description : BIX-01294 is a small molecule inhibitor of G9a and GLP (a H3K9 PKMT that shares 80% sequence identity with G9a in their respective SET domains) that was discovered via screening of a library of 125,000 synthetic compounds. BIX-01294 is selective for G9a and GLP over several H3K9 PKMTs including SUV39H1 and ESET, other KMTs such as SET7/9, and the arginine methyltransferase PRTM1. The X-ray crystal structure of GLP and BIX-01294 confirmed that BIX-01294 bound to the histone peptide binding pocket but failed to interact with the lysine binding channel. Cells dosed with BIX-01294 at 4.1 μM were characterized by reduced H3K9me2 levels in several cell lines but toxicity to cells at > 4.1 μM was observed.
Reference
William P. Janzen, Tim J. Wigle, Jian Jin, Stephen V. Frye. Epigenetics: tools and technologies. Drug Discov Today Technol. 2010 ; 7(1): 59 – 65.

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