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BIX 01294

Cat. No. 3364

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Chemical Name: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride

Biological Activity

G9a-like protein and G9a histone lysine methyltransferase inhibitor (IC₅₀ values are 0.7 and 1.7 μM respectively) that displays no activity at other histone methyltransferases up to 37 μM. Modulates H3K9me2 levels in mammalian cells and potentiates induction of pluripotent stem cells from somatic cells in vitro.

Technical Data

M.Wt:

600.02

Formula:

C₂₈H₃₈N₆O₂.3HCl

Solubility:

Soluble to 100 mM in water and to 100 mM in DMSO

Purity:

>98 %

Storage:

Desiccate at RT

CAS No:

935693-62-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Kubicek et al (2007) Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol.Cell 25 473. PMID: 17289593.

Shi et al (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3 568. PMID: 18983970.

Chang et al (2009) Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat.Struct.Mol.Biol. 16 312. PMID: 19219047.

Malmquist et al (2012) Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum. Proc.Natl.Acad.Sci.U S A 109 16708. PMID: 23011794.

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Keywords: BIX 01294, supplier, G9a-like, protein, and, G9a, histone, lysine, methyltransferases, HMTases, inhibitors, BIX01294, stem, cells, epigenetics