UNC 0642 (CAS 1481677-78-4)
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UNC 0642 is a selective and potent G9a and GLP inhibitor. It exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. UNC 0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50=110 nM). Histone methylation, specifically the methylation of lysine residues on histones, plays a role in determining the structure of euchromatin and regulating gene expression. Two important histone methyltransferases, G9a and G9a-like protein (GLP), are responsible for mono- or dimethylating lysine 9 on histone 3. This methylation process contributes significantly to early embryogenesis, genomic imprinting, and lymphocyte development.
UNC 0642 (CAS 1481677-78-4) References
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- Inhibition of lysine methyltransferase G9a/GLP reinstates long-term synaptic plasticity and synaptic tagging/capture by facilitating protein synthesis in the hippocampal CA1 area of APP/PS1 mouse model of Alzheimer's disease. | Han, JLT., et al. 2021. Transl Neurodegener. 10: 23. PMID: 34187583
- Detection of cancer stem cells by EMT-specific biomarker-based peptide ligands. | Chen, YA., et al. 2021. Sci Rep. 11: 22430. PMID: 34789743
- 7-Aminoalkoxy-Quinazolines from Epigenetic Focused Libraries Are Potent and Selective Inhibitors of DNA Methyltransferase 1. | Medina-Franco, JL., et al. 2022. Molecules. 27: PMID: 35566242
- Cholinergic REST-G9a gene repression through HMGB1-TLR4 neuroimmune signaling regulates basal forebrain cholinergic neuron phenotype. | Crews, FT. and Vetreno, RP. 2022. Front Mol Neurosci. 15: 992627. PMID: 36072299
- The mTORC1-G9a-H3K9me2 axis negatively regulates autophagy in fatty acid-induced hepatocellular lipotoxicity. | Mushtaq, A., et al. 2023. J Biol Chem. 299: 102937. PMID: 36690274
- Low level of antioxidant capacity biomarkers but not target overexpression predicts vulnerability to ROS-inducing drugs. | Samarin, J., et al. 2023. Redox Biol. 62: 102639. PMID: 36958250
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
UNC 0642, 10 mg | sc-397059 | 10 mg | $230.00 |