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Cat. No. Name Size Price Add Cart
KI1250BIX-0129410 mg$234
BIX-0129425 mg$432

Chemical Characteristic

Product NameBIX-01294
CAS No.935693-62-2
Molecular Weight 490.64
FormulaC28H38N6O2
Chemical NameN-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
Smilesn1c(nc(c2cc(c(cc12)OC)OC)NC1CCN(CC1)Cc1ccccc1)N1CCN(CCC1)C
Chemical Structure

Biological activities

BIX-01294 is a specific G9a histone methyltransferase inhibitor. BIX-01294 inhibits G9a and GLP with IC50 of 1.7 and 38 µM, respectively. BIX-01294 selectively impairs the G9a HMTase and the generation of H3K9me2 in vitro. BIX-01294 reduces H3K9me2 at several G9a target genes, including Tbc1d5, Alk, Serac1, Rb1, and Bmi1. BIX-01294 inhibits G9a in an uncompetitive manner with SAM, suggesting that it only bind to the enzyme-co-factor complex, but not the free enzyme. In vivo, BIX-01294 reduces H3K9me2 of bulk histones in several cell lines, including mouse ES cells, mouse embryonic fibroblasts (MEFs), and human HeLa cells. [1] Treatment of G9a-null cells with BIX-01294 results in decreased cell numbers. [2]

References

[1] Kubicek S, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007, 25(3): 473-481.
[2] Zheng YG, et al. Chemical regulation of epigenetic modifications: opportunities for new cancer therapy. Med Res Rev. 2008, 28(5): 645-687.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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