A potent and selective G9a HMTase inhibitor (IC50 = 15 nM

UNC0224 – 10 mg

Brand:
Cayman
CAS:
1197196-48-7
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} UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.{17642} Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).{17642}  

 

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Description

A potent and selective G9a HMTase inhibitor (IC50 = 15 nM, Kd = 23 mM); more than 1,000-fold selective for G9a over SET7/9 and SET8

Formal name: 7-[3-(dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine

Synonyms: 

Molecular weight: 485.7

CAS: 1197196-48-7

Purity: ≥98%

Formulation: A crystalline solid

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

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