A potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM

UNC0646 – 1 mg

Brand:
Cayman
CAS:
1320288-17-2
Storage:
-20
UN-No:
Non-Hazardous - /

G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).{19978} It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases.{19978} UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line.{19978} This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.{25782}  

 

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SKU: 11085 - 1 mg Category:

Description

A potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM)

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

Synonyms: 

Molecular weight: 621.9

CAS: 1320288-17-2

Purity: ≥95%

Formulation: A crystalline solid

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

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