B9311

BIX 01294 -trihydrochlorid Hydrat

≥98% (HPLC), powder

• Synonym(e): 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine -trihydrochlorid Hydrat
• Empirische Formel (Hill-System): C₂₈H₃₈N₆O₂·3HCl · xH₂O
• CAS-Nummer: 935693-62-2
• Molekulargewicht: 600.02 (anhydrous basis)
• MDL-Nummer: MFCD14560563
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Lagerbedingungen: desiccated
• Farbe: white
• Löslichkeit: H₂O: >20 mg/mL
• Lagertemp.: 2-8°C
• SMILES String: N2(CCC(CC2)Nc3nc(nc5c3cc(c(c5)OC)OC)N4CCN(CCC4)C)Cc1ccccc1
• InChI: 1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31)

Beschreibung

Allgemeine Beschreibung

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.

Anwendung

BIX 01294 trihydrochloride hydrate has been used:

• as a histone methylation inhibitor to treat E4 cells for analysing green fluorescent protein (d2EGFP) expression[1]
• to investigate the role of G9a in neuroblastoma tumor growth[2]
• 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[2]

Biochem./physiol. Wirkung

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.

Leistungsmerkmale und Vorteile

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Sonstige Hinweise

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable
• Persönliche Schutzausrüstung: Eyeshields, Gloves, type N95 (US)