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| Product | Description | |
|---|---|---|
| UNC0224 | The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM. Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase). Synonyms: UNC0224; UNC-0224; UNC 0224; 7-[3-(Dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine. Grades: >98%. CAS No. 1197196-48-7. Molecular formula: C26H43N7O2. Mole weight: 485.67. |  |
| HMTase Inhibitor V, UNC0224 (Histone Lysine Methyltransferase Inhibitor V, UNC0224, 7-(3-Dimethylaminopropoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine, H2O) | A quinazolinamine compound that acts as a potent, reversible and SAM (S-adenosylmethionine) non-competitive inhibitor of methyltransferases G9a (H3K9 HMT/EHMT2; IC50=15nM; =23nM) and GLP (G9a-like protein/EHMT1; IC50=20nM). Displays 1,000-fold greater selectivity for G9a over SET7/9 (H3K4 HMTase), SET8/PreSET7 (H4K20 HMTase), PRMT3 (MTase) and JMJD2E (demethylase), and minimally affects the activities of a broad range of GPCRs, ion-channels and transporters in a 30-target selectivity panel, with the exception of muscarinic M2 receptor and histamine H1 receptors (82% and 31% inhibition at 1uM, respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 1197196-48-7. Pack Sizes: 5mg. US Biological Life Sciences. |  Worldwide |
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