BIX-01294

Aliases: BIX-01294 3HCl, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride
Catalog No: 14072 Format: 25 mg $450 Buy
Catalog No: 14073 Format: 5 mg $100 Buy
Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 600.0
C28H38N6O2 3HCl
CAS 935693-62-2
>98% (TLC); NMR (Conforms)

Description

BIX-01294 is a selective inhibitor of G9a histone methyltransferase (IC50 = 1.7 µM) as well as GLP histone methyltransferase (IC50 = 38 µM) leading to a decrease in histone H3 lysine 9 methylation (H3K9me2) in vitro (ref 1). It facilitates the reactivation of pluripotency genes and induces passive demethylation, thus promoting reprogramming (ref 2). BIX-01294, in combination with BAY K8644 (a calcium channel agonist), was found to improve reprogramming efficiencies of Oct4-Klf4-(OK)-infected neural progenitor cells (ref 3). It induced apoptosis and decreased proliferation, mobility and invasion in human neuroblastoma cells (ref 4).

Contents

Off white crystalline solid. May be dissolved in DMSO (50 mg/ml); Water (50 mg/ml).

Storage Conditions

Store desiccated as supplied at room temperature for up to 2 years. Store solutions at -20°C for up to 3 months.

References

1. S Kubicek et al. Mol. Cell 2007, 25:473
2. D Huangfu et al. Nat. Biotechnol. 2008, 26:795
3. Y Shi et al. Cell Stem Cell 2008, 2:525
4. Z Lu et al. Anticancer Drugs 2013, 24:484

 
Chemical structure of BIX-01294 3HCl.

Chemical structure of BIX-01294 3HCl.