BIX 01294
BIX 01294 Basic information
- Product Name:
- BIX 01294
- Synonyms:
-
- BIX 01294 Trihydrochloride Hydrate
- 4-Quinazolinamine, 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-, hydrochloride (1:3)
- 2-(Hexahydro-4-Methyl-1H-1,4-Diazepin-1-yl)-6,7-Dimethoxy-[1-(Phenylmethyl)-4-Piperidynyl]-4-Quinazolinamine Trihydrochloride BIX01294 hydrochloride
- BIX01294 hydrochloride
- BIX01294 3hydrochloride
- Trihydrochloride Hydrate
- N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
- BIX 01204
- CAS:
- 1392399-03-9
- MF:
- C28H41Cl3N6O2
- MW:
- 600.02314
- Product Categories:
-
- Inhibitors
- Mol File:
- 1392399-03-9.mol
BIX 01294 Chemical Properties
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- H2O: >20mg/mL
- form
- powder
- color
- white
BIX 01294 Usage And Synthesis
Uses
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
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.
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.
in vivo
BIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited[1].
| Animal Model: | Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells[1] |
| Dosage: | 10 mg/kg |
| Administration: | IP; three times a week for 2 weeks |
| Result: | Significantly reduced tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth was not inhibited. Slowed the growth of orthotopic recurrent tumors in athymic nude recipients. |
storage
room temperature (desiccate)
BIX 01294Supplier
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