A potent

UNC0638 – 1 mg

Brand:
Cayman
CAS:
1255580-76-7
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} UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.{19269} See the Structural Genomics Consortium (SGC) website for more information.  

 

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SKU: 10734 - 1 mg Category:

Description

A potent, selective G9a and GLP HMTase inhibitor (IC50s = MB231 cells (IC50 = 81 nM) and demonstrates favorable separation of functional and toxic effects

Formal name: 2-cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine

Synonyms: 

Molecular weight: 509.7

CAS: 1255580-76-7

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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