A selective

GSK2879552 – 10 mg

Brand:
Cayman
CAS:
1401966-69-5
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.{31307} Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.{31307,31138} GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.{31307,31139}  

 

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Description

A selective, orally bioavailable, mechanism-based inactivator of LSD1/CoREST activity; enhances H3K4 methylation, increasing the expression of tumor-suppressor genes and preventing growth of AML cell lines (EC50s = 2-240 nM)

Formal name: 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-benzoic acid

Synonyms: 

Molecular weight: 364.5

CAS: 1401966-69-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Demethylation

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