An inhibitor of EZH2 (IC50 = 5.6 nM); selective for EZH2 over EZH1 (IC50 = 81 nM) and is greater than 4

ZLD1039 – 1 mg

Brand:
Cayman
CAS:
1826865-46-6
Storage:
-20
UN-No:
Non-Hazardous - /

ZLD1039 is an inhibitor of enhancer of zeste homolog 2 (EZH2; IC50 = 5.6 nM).{30588} It is 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. ZLD1039 also inhibits mutant Y641F and A677G EZH2 (IC50s = 15 and 4 nM, respectively, in a cell-free enzyme assay). It inhibits methylation of histone 3 lysine 27 (H3K27) in MCF-7 breast cancer cells (IC50 = 0.29 µM) and decreases expression of cadherin-1 (CDH1), cyclin-dependent kinase inhibitor 1C (CDKN1C), CDKN2A, and runt-related transcription factor 3 (RUNX3) in MCF-7 cells when used at concentrations of 1 and 2 µM. It also suppresses migration of MCF-7 cells when used at a concentration of 2 µM. ZLD1039 (200 mg/kg) reduces tumor growth in MCF-7 and MDA-MB-231 mouse xenograft models and inhibits tumor metastasis and decreases tumor protein levels of matrix metalloproteinase-2 (MMP-2), MMP-9, and E-cadherin in a 4T1 mouse xenograft model when administered at a dose of 250 mg/kg.  

 

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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

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