BIX-01294 (trihydrochloride)

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].

Product Specifications

CAS Number

[1392399-03-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Histone Methyltransferase

Type

Reference compound

Related Pathways

Autophagy; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bix-01294-trihydrochloride.html

Purity

99.68

Solubility

DMSO : 58.33 mg/mL (ultrasonic) |H2O : 100 mg/mL

Smiles

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

Molecular Formula

C28H41Cl3N6O2

Molecular Weight

600.02

Precautions

H302, H315, H319, H335

References & Citations

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