Description
An inhibitor of EZH2 (IC50 = 5.6 nM); selective for EZH2 over EZH1 (IC50 = 81 nM) and is greater than 4,700-fold selective for EZH2 in a panel of 14 histone methyltransferases; inhibits mutant Y641F and A677G EZH2 (IC50s = 15 and 4 nM, respectively); inhibits methylation of H3K27 in MCF-7 breast cancer cells (IC50 = 0.29 µM) and decreases expression of CDH1, CDKN1C, CDKN2A, and RUNX3 in MCF-7 cells at 1 and 2 µM; suppresses migration of MCF-7 cells at 2 µM; reduces tumor growth in MCF-7 and MDA-MB-231 mouse xenograft models at 200 mg/kg, and inhibits tumor metastasis and decreases tumor protein levels of MMP-2, MMP-9, and E-cadherin in a 4T1 mouse xenograft model at 250 mg/kg
Formal name: 3-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-N-[(2,3,5,6,7,8-hexahydro-1-methyl-3-oxo-4-isoquinolinyl)methyl]-2-methyl-5-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-benzamide
Synonyms:
Molecular weight: 612.8
CAS: 1826865-46-6
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Transcription Factors||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation
