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
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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.
- UPC:
- 51361501
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- B9311-5MG
