Histone Lysine Methyltransferase InhibidorAn HMTase inhibitor known as BIX-01294 Trihydrochloride

Histone Lysine Methyltransferase Inhibidor (CAS 935693-62-2 (hydrate))

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Sinónimo: BIX-01294
Solicitud: An HMTase inhibitor known as BIX-01294 Trihydrochloride
Número de CAS: 935693-62-2 (hydrate)
Pureza: >97%
Peso Molecular: 600
Fórmula Molecular: C28H38N6O2 3HCl
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Histone Lysine Methyltransferase Inhibitor (BIX-01294) is a G9a (histone lysine methyltransferase (HMTase)) inhibitor, specifically shown to inhibit the G9a-mediated generation of H3K9me2 (histone H3 lysine 9 dimethylation), not competitive with the S-adenosyl-methionine cofactor. Levels of H3K9me2 are restored with removal of BIX-01294. This molecule allows transient modulation of HMTase behavior, providing a tool for studying consequent effects on gene expression and chromatin organization. Histone Lysine Methyltransferase Inhibitor is an inhibitor of EHMT.


References

1. Kubicek, Stefan., et al., 2007. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Molecular cell. 25(3): 473-81. PMID: 17289593
2. Shi, Yan., et al., 2008. A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell stem cell. 2(6): 525-8. PMID: 18522845
3. Huangfu, Danwei., et al., 2008. Induction of pluripotent stem cells by defined factors is greatly improved by small-molecule compounds. Nature biotechnology. 26(7): 795-7. PMID: 18568017

Estado de Materia :
Solid
Solubilidad :
Soluble in water (100 mM), DMSO (5 mg/ml), and ethanol.
ALMACENAMIENTO :
Store at -20° C
Indice de Refracción :
n20D ~1.63 (Predicted)
IC50 :
G9a : IC50 = 0.11 µM (human); G9a-like protein: IC50 = 0.7 µM; EHMT: IC50 = 0.7 µM (human); G9a histone lysine methyltransferase: IC50 = 1.7 µM; GLP-catalyzed H3K9me3 : IC50 = 38 µM
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
PubChem CID :
25150857
Número MDL :
MFCD16618384
SMILES :
CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC

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Histone Lysine Methyltransferase Inhibidor  Menciones del Producto

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Citaciones 1 a 1 de un total de 1

PMID: # 27022024  Perez, RE. et al. 2016. J. Biol. Chem. 291: 10131-47.

Citaciones 1 a 1 de un total de 1
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