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B9311

Sigma-Aldrich

BIX 01294 trihydrochloride hydrate

≥98% (HPLC), powder

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Synonym(s):
2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride hydrate, BIX 01294
Empirical Formula (Hill Notation):
C28H38N6O2·3HCl · xH2O
Molecular Weight:
600.02 (anhydrous basis)
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

H2O: >20 mg/mL

storage temp.

2-8°C

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This Item
B5313PZ0115382190
BIX-01338 hydrate ≥98% (HPLC)

Sigma-Aldrich

B5313

BIX-01338 hydrate

form

powder

form

powder

form

-

form

solid

storage condition

desiccated

storage condition

-

storage condition

desiccated

storage condition

OK to freeze, protect from light

color

white

color

off-white to light tan

color

yellow

color

off-white

solubility

H2O: >20 mg/mL

solubility

DMSO: >10 mg/mL

solubility

H2O: ≥20 mg/mL

solubility

DMSO: 10 mg/mL, ethanol: 10 mg/mL

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

General description

BIX-01294, a diazepin-quinazolinamine derivative, is a histone-lysine methyltransferase (HMTase) inhibitor that modulates the epigenetic status of chromatin. BIX-01294 inhibits the G9aHMTase dependent levels of histone-3 lysine (9) methylation (H3K9me). Bix-01294 and valproic acid, a histone deacetylase (HDAC) inhibitor, may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes.

Application

BIX 01294 trihydrochloride hydrate has been used:
  • as a histone methylation inhibitor to treat E4 cells for analysing green fluorescent protein (d2EGFP) expression
  • to investigate the role of G9a in neuroblastoma tumor growth
  • as specific inhibitor of G9a to treat the SK-N-AS, BE(2)-C, SK-N-DZ, SK-N-F1, and SHEP1 neuroblastoma cell lines

Biochem/physiol Actions

BIX 01294 is a selective histone methyl transferase inhibitor. In its inhibition of the histone lysine methyltransferases, BIX 01294 does not compete with cofactor S-adenosyl-methionine. The target enzyme is G9a, and it selectively impairs G9a HMTase and the generation of H3K9me2 in vitro.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Other Notes

BIX-01294 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the BIX-01294 probe summary on the Chemical Probes Portal website.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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