BIX01294 hydrochloride A selective histone methyl transferase (HMTase) inhibitor.

BIX01294 hydrochloride (CAS 1392399-03-9)

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Sinónimo: 2-(Hexahydro-4-Methyl-1H-1,4-Diazepin-1-yl)-6,7-Dimethoxy-[1-(Phenylmethyl)-4-Piperidynyl]-4-Quinazolinamine Trihydrochloride
Solicitud: A selective histone methyl transferase (HMTase) inhibitor.
Número de CAS: 1392399-03-9
Pureza: ≥98%
Peso Molecular: 600.00
Fórmula Molecular: C28H38N6O23HCl
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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).

Estado de Materia :
Solid
Solubilidad :
Soluble in water (20 mg/ml).
ALMACENAMIENTO :
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)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
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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