A selective inhibitor of G9a histone methyltransferase (IC50 = 1.7 μM); less effectively inhibits G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known histone methyltransferases

BIX01294 (hydrochloride hydrate) – 1 mg

Brand:
Cayman
CAS:
1808255-64-2
Storage:
-20
UN-No:
Non-Hazardous - /

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.{17548,17546,17547} BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).{17550} It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.{17550} 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.{17549}  

 

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Description

A selective inhibitor of G9a histone methyltransferase (IC50 = 1.7 μM); less effectively inhibits G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known histone methyltransferases

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

Synonyms: 

Molecular weight: 600

CAS: 1808255-64-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cell Biology|Stem Cell Research|Reprogramming||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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