A-366 – 5 mg

Brand:
Cayman
CAS:
1527503-11-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM).{26028} It displays greater than 1,000-fold selectivity over 21 other methyltransferases.{26028} A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2.{26028} It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).{30715} See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM); significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells; also blocks the interaction of Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM)


Formal name: 5′-methoxy-6′-[3-(1-pyrrolidinyl)propoxy]-spiro[cyclobutane-1,3′-[3H]indol]-2′-amine

Synonyms: 

Molecular weight: 329.4

CAS: 1527503-11-2

Purity: ≥98%

Formulation: A crystalline solid


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