BIX-01294 trihydrochloride (Standard) 

BIX-01294 trihydrochloride (Standard) is the analytical standard of BIX-01294 (trihydrochloride) (HY-108239). This product is intended for research and analytical applications. BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells^{[1][2][3][4][5]}.

IC50: 2.7 μM (G9a in DELFIA assay)^[2]
IC50: 1.9 μM for G9a and 0.7 μM for GLP^[5]

600.02

C₂₈H₄₁Cl₃N₆O₂

1392399-03-9

CN(CCC1)CCN1C2=NC(C=C(OC)C(OC)=C3)=C3C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nathaniel W Mabe, et al. G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep. 2020 Nov 3;33(5):108341.  [Content Brief]

  [2]. Stefan Kubicek, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.  [Content Brief]

  [3]. Yang Q, et al. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012 Aug;45(4):335-44.  [Content Brief]

  [4]. Iwona Anna Ciechomska, et al. BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep  [Content Brief]

  [5]. Yanqi Chang, et al.Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol. 2009 Mar;16(3):312-7.  [Content Brief]