An EZH2 inhibitor (IC50 = 11.1 nM); colony formation of primary human CD34+ CML stem/progenitor cells at 0.5-5 µM; reduces global levels of H3K27me3 in K562 cells; induces regression of tumors in an EZH2-driven transgenic mouse model of lung adenocarcinoma at 75 mg/kg per day

JQEZ5 – 25 mg

Brand:
Cayman
CAS:
1913252-04-6
Storage:
-20
UN-No:
Non-Hazardous - /

JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).{48431,48432} It inhibits colony formation of primary human CD34+ chronic myelogenous leukemia (CML) stem/progenitor cells but not non-cancerous human CD34+ hematopoietic stem/progenitor cells when used at concentrations ranging from 0.5 to 5 µM.{48432} It also reduces global levels of trimethylated histone 3 lysine 27 (H3K27Me3), a mark that is regulated by PRC2, in K562 cells. JQEZ5 (75 mg/kg per day) induces regression of tumors in an EZH2-driven transgenic mouse model of lung adenocarcinoma.{48431}  

 

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SKU: 27457 - 25 mg Category:

Description

An EZH2 inhibitor (IC50 = 11.1 nM); colony formation of primary human CD34+ CML stem/progenitor cells at 0.5-5 µM; reduces global levels of H3K27me3 in K562 cells; induces regression of tumors in an EZH2-driven transgenic mouse model of lung adenocarcinoma at 75 mg/kg per day

Formal name: N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide

Synonyms: 

Molecular weight: 542.7

CAS: 1913252-04-6

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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