BIX 01294 [G9a/GLP HMTases Inhibitor]
[CAT#: MOD2005ZP73]
A highly potent, selective GLP / G9a HMTase inhibitor. A highly potentiates iPSC induction.
- Target:
- G9a / GLP HMTases
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Lot Number
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Description
A highly potent and selective G9a-like protein (GLP) and G9a histone lysine methyltransferase (HMTase) inhibitor (IC50 values of 0.7 and 1.9 µM, respectively). Exhibits anti-malarial and anti-cancer effects. It also enhance iPSC induction.
Synonyms
BIX-01294
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
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
B9-01294 (4.1 μM) treatment of G9anull ES cells resulted in a further reduction in H3K9me2 levels. BIX-01294 reduced H3K9me2 of several G9a target genes [1].
BIX-01294 (5 µM) reduces the level of overall H3K9 methylation in prokaryotic and 2-cell embryos. Embryos temporarily exposed to BIX-01294 have a reduced ability to establish pregnancy [2].
BIX-01294 (1 µg/mL) resulted in reduced BrdU incorporation of fetal PASMC. BIX-01294 treatment can reduce the migration of PASMCs induced by PDGF [3].
BIX-01294 (5 µM) reduces the level of overall H3K9 methylation in prokaryotic and 2-cell embryos. Embryos temporarily exposed to BIX-01294 have a reduced ability to establish pregnancy [2].
BIX-01294 (1 µg/mL) resulted in reduced BrdU incorporation of fetal PASMC. BIX-01294 treatment can reduce the migration of PASMCs induced by PDGF [3].
Reference
[1]. Kubicek S, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.
[2]. Park KE, et al. IVMBIX-01294, an inhibitor of the histone methyltransferase EHMT2, disrupts histone H3 lysine 9 (H3K9) dimethylation in the cleavage-stage porcine embryo. Reprod Fertil Dev. 2012;24(6):813-21.
[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.
[2]. Park KE, et al. IVMBIX-01294, an inhibitor of the histone methyltransferase EHMT2, disrupts histone H3 lysine 9 (H3K9) dimethylation in the cleavage-stage porcine embryo. Reprod Fertil Dev. 2012;24(6):813-21.
[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.
Molecular Weight
600.02
Form
Powder
Chemical Formula
C28H38N6O2.3HCl
Source
Synthetic
SMILES
CN(CCC3)CCN3C2=NC1=CC(OC)=C(OC)C=C1C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl
Solubility
Soluble in water (100mM) or DMSO (100mM)
IC50
1.9 μM (G9a Histone Methyltransferase)
CAS NO.
1392399-03-9
PubChem Substance ID
46945860
Purity
>98%
Storage
Room temperature (desiccate)
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -27°C for several months.
Research Use Only
For research use only
Target
G9a / GLP HMTases
Official Name
G9a / GLP HMTases
Alternative Names
G9a / GLP HMTases
For Research Use Only. Not For Clinical Use.
