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BIX 01294

(HB1413)
Data

Product overview

  • Name
    BIX 01294
  • Short description
    Potent, selective GLP / G9a HMTase inhibitor. Potentiates iPSC induction.
  • Biological description
    Potent and selective G9a-like protein (GLP) and G9a histone lysine methyltransferase (HMTase) inhibitor (IC50 values are 0.7 and 1.9 µM respectively). Shows antimalarial and anti-cancer actions. Also potentiates iPSC induction.
  • Alternative names
    BIX-01294
  • Biological action
    Inhibitor
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    2-(Hexahydro-4-methyl-1H-1,4-diazep in-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piper idinyl]-4-quinazolinamine trihydrochloride
  • Molecular Weight
    600.02
  • Chemical structure
    BIX 01294  [1392399-03-9]
  • Molecular Formula
    C28H38N6O2.3HCl
  • CAS Number
    1392399-03-9

Storing and Using Your Product

  • Storage instructions
    room temperature (desiccate)
  • Solubility overview
    soluble in water (100mM) or DMSO (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for BIX 01294

  • Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.

    Kubicek S et al (2007) Mol Cell 25(3) : 473-81.
    PubMedID: 17289593
  • Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum.

    Malmquist NA et al (2012) Proc Natl Acad Sci U S A 109(41) : 16708-13.
    PubMedID: 23011794
  • Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.

    Chang Y et al (2009) Nat Struct Mol Biol 16(3) : 312-7.
    PubMedID: 19219047
  • Euchromatic histone methyltransferase 2 inhibitor, BIX-01294, sensitizes human promyelocytic leukemia HL-60 and NB4 cells to growth inhibition and differentiation.

    Savickiene J et al (2014) Leuk Res 38(7) : 822-9.
    PubMedID: 24832370
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