Product overview

Name BIX 01294
Alternative names BIX-01294
Purity >98%
Description Potent, selective GLP / G9a HMTase inhibitor. Potentiates iPSC induction.
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Biological Data

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.

Solubility & Handling

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.

Calculators

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Chemical Data

Purity >98%
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] Chemical Structure
Molecular Formula C28H38N6O2.3HCl
CAS Number 1392399-03-9
PubChem identifier 46945860
SMILES CN(CCC3)CCN3C2=NC1=CC(OC)=C(OC)C=C1C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl
InChiKey FMURUEPQXKJIPS-UHFFFAOYSA-N

References for BIX 01294

References are publications that support the biological activity of the product
  • 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.
  • 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.
  • 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.
  • Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.

    Kubicek S et al (2007) Mol Cell 25(3) : 473-81.

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