BIX01294 hydrochlorideA selective histone methyl transferase (HMTase) inhibitor.

BIX01294 hydrochloride (CAS 1392399-03-9)

BIX01294 hydrochloride | CAS 1392399-03-9 is rated 5.0 out of 5 by 1.
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Synonym: 2-(Hexahydro-4-Methyl-1H-1,4-Diazepin-1-yl)-6,7-Dimethoxy-[1-(Phenylmethyl)-4-Piperidynyl]-4-Quinazolinamine Trihydrochloride
Application: A selective histone methyl transferase (HMTase) inhibitor.
CAS Number: 1392399-03-9
Purity: ≥98%
Molecular Weight: 600.00
Molecular Formula: C28H38N6O23HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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BIX01294 hydrochloride inhibits G9a. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 hydrochloride is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 hydrochloride has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro. BIX01294 hydrochloride is an inhibitor of HDAC.


References

1 Tachibana, M., Sugimoto, K., Nozaki, M., et al. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis. Genes Dev 16 1779-1791 (2002). 2 Wagschal, A., Sutherland, H.G., Woodfine, K., et al. G9a histone methyltransferase contributes to imprinting in the mouse placenta. Mol Cell Biol 28(3) 1104-1113 (2008). 3 Thomas, L.R., Miyashita, H., Cobb, R.M., et al. Functional analysis of histone methyltransferase G9a in B and T lymphocytes. J Immunol 181 485-493 (2008). 4 Kubicek, S., O′Sullivan, R.J., August, E.M., et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Molecular Cell 25 473-481 (2007). 5 Shi, Y., Desponts, C., Do, J.T., et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3(5) 568-574 (2008).

Physical State :
Solid
Solubility :
Soluble in water (20 mg/ml).
Storage :
Store at -20° C
IC50 :
G9a HMTase: IC50 = 1.7 µM; HMTase G9a-like protein: IC50 = 38 µM; Histone-lysine N-methyltransferase, H3 lysine-9 specific 5: IC50 = 27 nM (human); Histone-lysine N-methyltransferase, H3 lysine-9 specific 3: IC50 = 110 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
46945860
SMILES :
CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC.Cl.Cl.Cl

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Certificate of Analysis

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Rated 5 out of 5 by from Chen et al Chen et al. (PubMed ID 26285804) found that the histone methyltransferase inhibitor, BIX01294 hydrochloride, decreased H3K9 dimethylation in Snrpn mouse embryonic fibroblasts. -SCBT Publication Review
Date published: 2015-02-15
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