A selective EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50s = 15 and 13 nM

EI1 – 5 mg

Brand:
Cayman
CAS:
1418308-27-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2 (PRC2), catalyzes trimethylation of lysine 27 on histone H3 (H3K27) and is involved in proliferation and aggressive cell growth associated with neoplastic cells.{18930} EI1 is an EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50s = 15 and 13 nM, respectively).{30943} It displays 90-fold selectivity for EZH2 over EZH1 and >10,000-fold over other lysine methyltransferases. EI1 blocks cellular H3K27 methylation and activates PRC2-specific gene expression.{30943} Inhibition of EZH2 by EI1 in diffused large B cell lymphoma cells carrying Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis.{30943}  

 

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Description

A selective EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50s = 15 and 13 nM, respectively); blocks cellular H3K27 methylation and activates PRC2-specific gene expression; decreases proliferation, cell cycle arrest, and apoptosis in diffused large B cell lymphoma cells carrying Y641 mutations

Formal name: 6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide

Synonyms: 

Molecular weight: 390.5

CAS: 1418308-27-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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