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BIX 01294

BIX 01294

Catalog Number:
L002368352APE
Mfr. No.:
APE-A1909
Price:
$273
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      • Overview

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          Background

          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.

      • Properties
        • Alternative Name
          N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
          CAS Number
          935693-62-2
          Molecular Formula
          C28H38N6O2
          Molecular Weight
          490.65
          Appearance
          A solid
          Purity
          99.56%
          Solubility
          ≥24.45 mg/mL in DMSO; ≥5.1 mg/mL in EtOH with ultrasonic; ≥51.2 mg/mL in H2O
          Storage
          Store at -20°C

          * For Research Use Only

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