• 产品描述： 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

• 靶点： IC50: 2.7 μM (G9a in DELFIA assay) IC50: 1.9 μM for G9a and 0.7 μM for GLP;HistoneMethyltransferase; Autophagy

• 体内研究：
  BIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited. Animal Model: Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells Dosage: 10 mg/kg Administration: IP; three times a week for 2 weeks Result: Significantly reduced tumor growth and tumor burden in recurrent tumor cells.Primary tumor growth was not inhibited.Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.

• 参考文献：
  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.

• 保存条件： RT

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.667 ml	8.333 ml	16.666 ml
  5 mM	0.333 ml	1.667 ml	3.333 ml
  10 mM	0.167 ml	0.833 ml	1.667 ml
  50 mM	0.033 ml	0.167 ml	0.333 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *