BIX01294 (hydrochloride hydrate)

Product Name: BIX01294 (hydrochloride hydrate)
CAS No.: 1808255-64-2
Chemical Name: BIX01294 (hydrochloride hydrate)
Synonyms: BIX01294 (hydrochloride hydrate);BIX01294 (hydrochloride hydrate),BIX-01294 (hydrochloride hydrate);N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine hydrate trihydrochloride;2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine,trihydrochloride,hydrate
CBNumber: CB72590339
Molecular Formula: C28H41ClN6O3
Formula Weight: 545.13
MOL File: 1808255-64-2.mol

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BIX01294 (hydrochloride hydrate) Property

storage temp.: Store at -20°C
solubility: DMSO: 5 mg/ml; Water: 10 mg/ml
form: A crystalline solid

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 13124
Product name: BIX01294 (hydrochloride hydrate)
Purity: ≥98%
Packaging: 1mg
Price: $30
Updated: 2024/03/01

Cayman Chemical

Product number: 13124
Product name: BIX01294 (hydrochloride hydrate)
Purity: ≥98%
Packaging: 5mg
Price: $113
Updated: 2024/03/01

Cayman Chemical

Product number: 13124
Product name: BIX01294 (hydrochloride hydrate)
Purity: ≥98%
Packaging: 10mg
Price: $169
Updated: 2024/03/01

Cayman Chemical

Product number: 13124
Product name: BIX01294 (hydrochloride hydrate)
Purity: ≥98%
Packaging: 50mg
Price: $558
Updated: 2024/03/01

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BIX01294 (hydrochloride hydrate) Chemical Properties,Usage,Production

Description

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.^1,2,3 BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC₅₀ = 1.7 μM).⁴ It less effectively inhibits the HMTase G9a-like protein (GLP; IC₅₀ = 38 μM) and has no effect on other known HMTases.⁴ BIX01294 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.⁵

Uses

BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells[1][2].

IC 50

G9a: 1.7 μM (IC₅₀); GLP: 38 μM (IC₅₀)

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(14),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(1),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 Mol. 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).

BIX01294 (hydrochloride hydrate) Preparation Products And Raw materials

Raw materials

Preparation Products

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1808255-64-2, BIX01294 (hydrochloride hydrate)Related Search:

BIX01294 (hydrochloride hydrate)

BIX01294 (hydrochloride hydrate),BIX-01294 (hydrochloride hydrate)

2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine,trihydrochloride,hydrate

N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine hydrate trihydrochloride

1808255-64-2