ZLD1039 |
Catalog No.GC45609 |
ZLD1039 est un inhibiteur EZH2 puissant, hautement sélectif et biodisponible par voie orale. ZLD1039 montre une inhibition puissante et dépendante de la concentration de l'activité enzymatique de PRC2 contre le type sauvage EZH2 ainsi que les enzymes mutantes Y641F et A677G avec des valeurs IC50 de 5, 6, 15 et 4, 0 nM, respectivement. Le ZLD1039 inhibe la croissance et les métastases des tumeurs mammaires.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1826865-46-6
Sample solution is provided at 25 µL, 10mM.
ZLD1039 is an inhibitor of enhancer of zeste homolog 2 (EZH2; IC50 = 5.6 nM).1 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.
|1. Song, X., Gao, T., Wang, N., et al. Selective inhibition of EZH2 by ZLD1039 blocks H3K27methylation and leads to potent anti-tumor activity in breast cancer. Sci.Rep. 6:20864, (2016).
Average Rating: 5
(Based on Reviews and 26 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *